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Nanomedicine Based Drug Delivery Systems: Recent Developments and Future Prospects

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 December 2022) | Viewed by 51842

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Guest Editor
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
Interests: bioavailability; nanomedicine; nanoemulsion; SNEDDS; solubilization; transdermal drug delivery system
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Special Issue Information

Dear Colleagues,

Since the discovery of nanomedicine-based drug delivery carriers such as nanoparticles, liposomes, and self-nanoemulsifying drug delivery systems (SNEDDS), enormous progress has been achieved in the field of innovative active biomolecule drug delivery systems. The use of nanomedicines as drug delivery carriers has garnered a lot of interest in recent years for the therapeutic targeting of specific cells. Biocompatibility, biodegradability, low toxicity, drug delivery efficiency, drug targeting efficiency, and improved solubility, bioavailability, and bioactivities are all advantages of these nanosized drug delivery carriers. Furthermore, these carriers can encapsulate a diverse range of active therapeutic biomolecules. These nanomedicine-based drug delivery carriers can also improve the pharmacokinetic and pharmacodynamics efficiencies of active therapeutic biomolecules, allowing for a more sustained, targeted, and controlled drug delivery system. Various studies have recently shown progress in nanomedicine-based drug delivery systems for future therapeutic targeting. This Special Issue aims to collect recent advances, developments, and future prospects on the design, development, characterization, and biological evaluation of nanomedicine-based drug delivery systems for active therapeutic biomolecules.

Dr. Faiyaz Shakeel
Guest Editor

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Keywords

  • Carbon nanotubes
  • Liposomes
  • Metallic nanoparticles
  • Nanocarriers
  • Nanoemulsions
  • Nanostructured lipid carriers
  • Niosomes
  • Polymeric nanoparticles
  • Solid lipid nanoparticles
  • Self-nanoemulsifying drug delivery systems

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Published Papers (14 papers)

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Editorial

Jump to: Research, Review

3 pages, 158 KiB  
Editorial
Editorial: Nanomedicine-Based Drug Delivery Systems: Recent Developments and Future Prospects
by Faiyaz Shakeel
Molecules 2023, 28(10), 4138; https://doi.org/10.3390/molecules28104138 - 17 May 2023
Cited by 6 | Viewed by 1559
Abstract
Since the discovery of nanomedicine-based drug delivery carriers such as nanoparticles, liposomes, and self-nanoemulsifying drug delivery systems (SNEDDS), enormous progress has been achieved in the field of innovative active biomolecule drug delivery systems [...] Full article

Research

Jump to: Editorial, Review

14 pages, 2290 KiB  
Article
Erlotinib-Loaded Dendrimer Nanocomposites as a Targeted Lung Cancer Chemotherapy
by Wafa K. Fatani, Fadilah S. Aleanizy, Fulwah Y. Alqahtani, Mohammed M. Alanazi, Abdullah A. Aldossari, Faiyaz Shakeel, Nazrul Haq, Hosam Abdelhady, Hamad M. Alkahtani and Ibrahim A. Alsarra
Molecules 2023, 28(9), 3974; https://doi.org/10.3390/molecules28093974 - 8 May 2023
Cited by 17 | Viewed by 2658
Abstract
Lung cancer is the main cause of cancer-related mortality globally. Erlotinib is a tyrosine kinase inhibitor, affecting both cancerous cell proliferation and survival. The emergence of oncological nanotechnology has provided a novel drug delivery system for erlotinib. The aims of this current investigation [...] Read more.
Lung cancer is the main cause of cancer-related mortality globally. Erlotinib is a tyrosine kinase inhibitor, affecting both cancerous cell proliferation and survival. The emergence of oncological nanotechnology has provided a novel drug delivery system for erlotinib. The aims of this current investigation were to formulate two different polyamidoamine (PAMAM) dendrimer generations—generation 4 (G4) and generation 5 (G5) PAMAM dendrimer—to study the impact of two different PAMAM dendrimer formulations on entrapment by drug loading and encapsulation efficiency tests; to assess various characterizations, including particle size distribution, polydispersity index, and zeta potential; and to evaluate in vitro drug release along with assessing in situ human lung adenocarcinoma cell culture. The results showed that the average particle size of G4 and G5 nanocomposites were 200 nm and 224.8 nm, with polydispersity index values of 0.05 and 0.300, zeta potential values of 11.54 and 4.26 mV of G4 and G5 PAMAM dendrimer, respectively. Comparative in situ study showed that cationic G4 erlotinib-loaded dendrimer was more selective and had higher antiproliferation activity against A549 lung cells compared to neutral G5 erlotinib-loaded dendrimers and erlotinib alone. These conclusions highlight the potential effect of cationic G4 dendrimer as a targeting-sustained-release carrier for erlotinib. Full article
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16 pages, 1226 KiB  
Article
Perspectives of Positively Charged Nanocrystals of Tedizolid Phosphate as a Topical Ocular Application in Rabbits
by Abdullah Alshememry, Musaed Alkholief, Mohd Abul Kalam, Mohammad Raish, Raisuddin Ali, Sulaiman S. Alhudaithi, Muzaffar Iqbal and Aws Alshamsan
Molecules 2022, 27(14), 4619; https://doi.org/10.3390/molecules27144619 - 20 Jul 2022
Cited by 6 | Viewed by 1980
Abstract
The aim of this study was the successful utilization of the positively charged nanocrystals (NCs) of Tedizolid Phosphate (TZP) (0.1% w/v) for topical ocular applications. TZP belongs to the 1, 3-oxazolidine-2-one class of antibiotics and has therapeutic potential for the [...] Read more.
The aim of this study was the successful utilization of the positively charged nanocrystals (NCs) of Tedizolid Phosphate (TZP) (0.1% w/v) for topical ocular applications. TZP belongs to the 1, 3-oxazolidine-2-one class of antibiotics and has therapeutic potential for the treatment of many drug-resistant bacterial infections, including eye infections caused by MRSA, penicillin-resistant Streptococcus pneumonia and vancomycin-resistant Enterococcus faecium. However, its therapeutic usage is restricted due to its poor aqueous solubility and limited ocular availability. It is a prodrug and gets converted to Tedizolid (TDZ) by phosphatases in vivo. The sterilized NC1 was subjected to antimicrobial testing on Gram-positive bacteria. Ocular irritation and pharmacokinetics were performed in rabbits. Around a 1.29 to 1.53-fold increase in antibacterial activity was noted for NC1 against the B. subtilis, S. pneumonia, S. aureus and MRSA (SA-6538) as compared to the TZP-pure. The NC1-AqS was “practically non-irritating” to rabbit eyes. There was around a 1.67- and 1.43 fold increase in t1/2 (h) and Cmax (ngmL−1) while there were 1.96-, 1.91-, 2.69- and 1.41-times increases in AUC0–24h,AUC0–∞,AUMC0–∞ and MRT0–∞, respectively, which were found by NC1 as compared to TZP-AqS in the ocular pharmacokinetic study. The clearance of TDZ was faster (11.43 mLh−1) from TZP-AqS as compared to NC1 (5.88 mLh−1). Relatively, an extended half-life (t1/2; 4.45 h) of TDZ and the prolonged ocular retention (MRT0–∞; 7.13 h) of NC1 was found, while a shorter half-life (t1/2; 2.66 h) of TDZ and MRT0–∞(t1/2; 5.05 h)was noted for TZP-AqS, respectively. Cationic TZP-NC1 could offer increased transcorneal permeation, which could mimic the improved ocular bioavailability of the drug in vivo. Conclusively, NC1 of TZP was identified as a promising substitute for the ocular delivery of TZP, with better performance as compared to its conventional AqS. Full article
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13 pages, 21390 KiB  
Article
Novel C60 Fullerenol-Gentamicin Conjugate–Physicochemical Characterization and Evaluation of Antibacterial and Cytotoxic Properties
by Aleksandra Nurzynska, Piotr Piotrowski, Katarzyna Klimek, Julia Król, Andrzej Kaim and Grazyna Ginalska
Molecules 2022, 27(14), 4366; https://doi.org/10.3390/molecules27144366 - 7 Jul 2022
Cited by 8 | Viewed by 2118
Abstract
This study aimed to develop, characterize, and evaluate antibacterial and cytotoxic properties of novel fullerene derivative composed of C60 fullerenol and standard aminoglycoside antibiotic–gentamicin (C60 fullerenol-gentamicin conjugate). The successful introduction of gentamicin to fullerenol was confirmed by X-ray photoelectron spectroscopy which [...] Read more.
This study aimed to develop, characterize, and evaluate antibacterial and cytotoxic properties of novel fullerene derivative composed of C60 fullerenol and standard aminoglycoside antibiotic–gentamicin (C60 fullerenol-gentamicin conjugate). The successful introduction of gentamicin to fullerenol was confirmed by X-ray photoelectron spectroscopy which together with thermogravimetric and spectroscopic analysis revealing the formula of the composition as C60(OH)12(GLYMO)11(Gentamicin)0.8. The dynamic light scattering (DLS) revealed that conjugate possessed ability to form agglomerates in water (size around 115 nm), while Zeta potential measurements demonstrated that such agglomerates possessed neutral character. In vitro biological assays indicated that obtained C60 fullerenol-gentamicin conjugate possessed the same antibacterial activity as standard gentamicin against Staphylococcus aureus, Staphylococcus epidermidis, Pseudomonas aeruginosa, and Escherichia coli, which proves that combination of fullerenol with gentamicin does not cause the loss of antibacterial activity of antibiotic. Moreover, cytotoxicity assessment demonstrated that obtained fullerenol-gentamicin derivative did not decrease viability of normal human fibroblasts (model eukaryotic cells) compared to control fibroblasts. Thus, taking into account all of the results, it can be stated that this research presents effective method to fabricate C60 fullerenol-gentamicin conjugate and proves that such derivative possesses desired antibacterial properties without unfavorable cytotoxic effects towards eukaryotic cells in vitro. These promising preliminary results indicate that obtained C60 fullerenol-gentamicin conjugate could have biomedical potential. It may be presumed that obtained fullerenol may be used as an effective carrier for antibiotic, and developed fullerenol-gentamicin conjugate may be apply locally (i.e., at the wound site). Moreover, in future we will evaluate possibility of its applications in inter alia tissue engineering, namely as a component of wound dressings and implantable biomaterials. Full article
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19 pages, 1797 KiB  
Article
Self-Nanoemulsifying Drug Delivery System (SNEDDS) of Apremilast: In Vitro Evaluation and Pharmacokinetics Studies
by Ahad S. Abushal, Fadilah S. Aleanizy, Fulwah Y. Alqahtani, Faiyaz Shakeel, Muzaffar Iqbal, Nazrul Haq and Ibrahim A. Alsarra
Molecules 2022, 27(10), 3085; https://doi.org/10.3390/molecules27103085 - 11 May 2022
Cited by 17 | Viewed by 3392
Abstract
Psoriatic arthritis is an autoimmune disease of the joints that can lead to persistent inflammation, irreversible joint damage and disability. The current treatments are of limited efficacy and inconvenient. Apremilast (APR) immediate release tablets Otezla® have 20–33% bioavailability compared to the APR [...] Read more.
Psoriatic arthritis is an autoimmune disease of the joints that can lead to persistent inflammation, irreversible joint damage and disability. The current treatments are of limited efficacy and inconvenient. Apremilast (APR) immediate release tablets Otezla® have 20–33% bioavailability compared to the APR absolute bioavailability of 73%. As a result, self-nanoemulsifying drug delivery systems (SNEDDS) of APR were formulated to enhance APR’s solubility, dissolution, and oral bioavailability. The drug assay was carried out using a developed and validated HPLC method. Various thermodynamic tests were carried out on APR-SNEDDS. Stable SNEDDS were characterized then subjected to in vitro drug release studies via dialysis membrane. The optimum formulation was F9, which showed the maximum in vitro drug release (94.9%) over 24 h, and this was further investigated in in vivo studies. F9 was composed of 15% oil, 60% Smix, and 25% water and had the lowest droplet size (17.505 ± 0.247 nm), low PDI (0.147 ± 0.014), low ZP (−13.35 mV), highest %T (99.15 ± 0.131) and optimum increases in the relative bioavailability (703.66%) compared to APR suspension (100%) over 24 h. These findings showed that APR-SNEDDS is a possible alternative delivery system for APR. Further studies are warranted to evaluate the major factors that influence the encapsulation efficiency and stability of APR-containing SNEDDS. Full article
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12 pages, 1921 KiB  
Article
Levonorgestrel Microneedle Array Patch for Sustained Release Contraception: Formulation, Optimization and In Vivo Characterization
by Amarjitsing Rajput, Riyaz Ali M. Osmani, Achyut Khire, Sanket Jaiswal and Rinti Banerjee
Molecules 2022, 27(7), 2349; https://doi.org/10.3390/molecules27072349 - 6 Apr 2022
Cited by 13 | Viewed by 4143
Abstract
Background: The goal of this work was to develop a levonorgestrel liposome-loaded microneedle array patch for contraception. Methods: Levonorgestrel-loaded liposome was formulated by a solvent injection technique, characterized, and studied. Results: The formulated liposomes were characterized for particle size (147 ± 8 nm), [...] Read more.
Background: The goal of this work was to develop a levonorgestrel liposome-loaded microneedle array patch for contraception. Methods: Levonorgestrel-loaded liposome was formulated by a solvent injection technique, characterized, and studied. Results: The formulated liposomes were characterized for particle size (147 ± 8 nm), polydispersity index (0.207 ± 0.03), zeta potential (−23 ± 4.25 mV), drug loading (18 ± 3.22%) and entrapment efficiency (85 ± 4.34%). A cryo high-resolution transmission electron microscopy and cryo field emission gun scanning electron microscopy study showed spherical shaped particles with a smooth surface. The in vitro drug release and in vivo pharmacokinetic study showed sustained behaviour of Levonorgestrel for 28 days. Conclusion: The levonorgestrel liposome-loaded microneedle array patch showed better contraception than the drug-loaded microneedle array patch. Full article
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22 pages, 2560 KiB  
Article
Development and Evaluation of Chitosan Nanoparticles for Ocular Delivery of Tedizolid Phosphate
by Mohd Abul Kalam, Muzaffar Iqbal, Abdullah Alshememry, Musaed Alkholief and Aws Alshamsan
Molecules 2022, 27(7), 2326; https://doi.org/10.3390/molecules27072326 - 4 Apr 2022
Cited by 23 | Viewed by 3206
Abstract
This study investigates the development of topically applied non-invasive chitosan-nanoparticles (CSNPs) for ocular delivery of tedizolid phosphate (TZP) for the treatment of MRSA-related ocular and orbital infections. An ionic-gelation method was used to prepare TZP-encapsulated CSNPs using tripolyphosphate-sodium (TPP) as cross-linker. Particle characterization [...] Read more.
This study investigates the development of topically applied non-invasive chitosan-nanoparticles (CSNPs) for ocular delivery of tedizolid phosphate (TZP) for the treatment of MRSA-related ocular and orbital infections. An ionic-gelation method was used to prepare TZP-encapsulated CSNPs using tripolyphosphate-sodium (TPP) as cross-linker. Particle characterization was performed by the DLS technique (Zeta-Sizer), structural morphology was observed by SEM. The drug encapsulation and loading were determined by the indirect method. In-vitro release was conducted through dialysis bags in simulated tear fluid (pH 7) with 0.25% Tween-80. Physicochemical characterizations were performed for ocular suitability of CSNPS. An antimicrobial assay was conducted on different strains of Gram-positive bacteria. Eye-irritation from CSNPs was checked in rabbits. Transcorneal flux and apparent permeability of TZP from CSNPs was estimated through excised rabbit cornea. Ionic interaction between the anionic and cationic functional groups of TPP and CS, respectively, resulted in the formation of CSNPs at varying weight ratios of CS/TPP with magnetic stirring (700 rpm) for 4 h. The CS/TPP weight ratio of 3.11:1 with 10 mg of TZP resulted in optimal-sized CSNPs (129.13 nm) with high encapsulation (82%) and better drug loading (7%). Release profiles indicated 82% of the drug was released from the TZP aqueous suspension (TZP-AqS) within 1 h, while it took 12 h from F2 to release 78% of the drug. Sustained release of TZP from F2 was confirmed by applying different release kinetics models. Linearity in the profile (suggested by Higuchi’s model) indicated the sustained release property CSNPs. F2 has shown significantly increased (p < 0.05) antibacterial activity against some Gram-positive strains including one MRSA strain (SA-6538). F2 exhibited a 2.4-fold increased transcorneal flux and apparent permeation of TZP as compared to TZP-AqS, indicating the better corneal retention. No sign or symptoms of discomfort in the rabbits’ eyes were noted during the irritation test with F2 and blank CSNPs, indicating the non-irritant property of the TZP-CSNPs. Thus, the TZP-loaded CSNPs have strong potential for topical use in the treatment of ocular MRSA infections and related inflammatory conditions. Full article
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17 pages, 3399 KiB  
Article
Pharmaceutical Development and Design of Thermosensitive Liposomes Based on the QbD Approach
by Dorina Gabriella Dobó, Zsófia Németh, Bence Sipos, Martin Cseh, Edina Pallagi, Dániel Berkesi, Gábor Kozma, Zoltán Kónya and Ildikó Csóka
Molecules 2022, 27(5), 1536; https://doi.org/10.3390/molecules27051536 - 24 Feb 2022
Cited by 7 | Viewed by 3079
Abstract
This study aimed to produce thermosensitive liposomes (TSL) by applying the quality by design (QbD) concept. In this paper, our research group collected and studied the parameters that significantly impact the quality of the liposomal product. Thermosensitive liposomes are vesicles used as drug [...] Read more.
This study aimed to produce thermosensitive liposomes (TSL) by applying the quality by design (QbD) concept. In this paper, our research group collected and studied the parameters that significantly impact the quality of the liposomal product. Thermosensitive liposomes are vesicles used as drug delivery systems that release the active pharmaceutical ingredient in a targeted way at ~40–42 °C, i.e., in local hyperthermia. This study aimed to manufacture thermosensitive liposomes with a diameter of approximately 100 nm. The first TSLs were made from DPPC (1,2-dipalmitoyl-sn-glycerol-3-phosphocholine) and DSPC (1,2-dioctadecanoyl-sn-glycero-3-phosphocholine) phospholipids. Studies showed that the application of different types and ratios of lipids influences the thermal properties of liposomes. In this research, we made thermosensitive liposomes using a PEGylated lipid besides the previously mentioned phospholipids with the thin-film hydration method. Full article
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15 pages, 2855 KiB  
Article
Design of Turmeric Rhizome Extract Nano-Formula for Delivery to Cancer Cells
by Sakchai Auychaipornlert, Pojawon Prayurnprohm Lawanprasert, Suchada Piriyaprasarth, Pongtip Sithisarn and Supachoke Mangmool
Molecules 2022, 27(3), 896; https://doi.org/10.3390/molecules27030896 - 28 Jan 2022
Cited by 6 | Viewed by 2731
Abstract
Novel turmeric rhizome extract nanoparticles (TE-NPs) were developed from fractions of dried turmeric (Curcuma longa Linn.) rhizome. Phytochemical studies, by using HPLC and TLC, of the fractions obtained from ethanol extraction and solvent–solvent extraction showed that turmeric rhizome ethanol extract (EV) and [...] Read more.
Novel turmeric rhizome extract nanoparticles (TE-NPs) were developed from fractions of dried turmeric (Curcuma longa Linn.) rhizome. Phytochemical studies, by using HPLC and TLC, of the fractions obtained from ethanol extraction and solvent–solvent extraction showed that turmeric rhizome ethanol extract (EV) and chloroform fraction (CF) were composed mainly of three curcuminoids and turmeric oil. Hexane fraction (HE) was composed mainly of turmeric oil while ethyl acetate fraction (EA) was composed mainly of three curcuminoids. The optimal TE-NPs formulation with particle size of 159.6 ± 1.7 nm and curcumin content of 357.48 ± 8.39 µM was successfully developed from 47-run D-optimal mixture–process variables experimental design. Three regression models of z-average, d50, and d90 could be developed with a reasonable accuracy of prediction (predicted r2 values were in the range of 0.9120–0.9992). An in vitro cytotoxicity study using MTT assay demonstrated that the optimal TE-NPs remarkably exhibited the higher cytotoxic effect on human hepatoma cells, HepG2, when compared with free curcumin. This study is the first to report nanoparticles prepared from turmeric rhizome extract and their cytotoxic activity to hepatic cancer cells compared with pure curcumin. These nanoparticles might serve as a potential delivery system for cancer therapy. Full article
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12 pages, 1679 KiB  
Article
Enhancing Ocular Bioavailability of Ciprofloxacin Using Colloidal Lipid-Based Carrier for the Management of Post-Surgical Infection
by Fakhria A. Al-Joufi, Mounir M. Salem-Bekhit, Ehab I. Taha, Mohamed A. Ibrahim, Magdy M. Muharram, Sultan Alshehri, Mohammed M. Ghoneim and Faiyaz Shakeel
Molecules 2022, 27(3), 733; https://doi.org/10.3390/molecules27030733 - 23 Jan 2022
Cited by 13 | Viewed by 3048
Abstract
Conjunctivitis and endogenous bacterial endophthalmitis mostly occurred after ophthalmic surgery. Therefore, the present study aimed to maximize the ocular delivery of ciprofloxacin (CPX) using colloidal lipid-based carrier to control the post-surgical infection. In this study, CPX was formulated as ophthalmic liposomal drops. Two [...] Read more.
Conjunctivitis and endogenous bacterial endophthalmitis mostly occurred after ophthalmic surgery. Therefore, the present study aimed to maximize the ocular delivery of ciprofloxacin (CPX) using colloidal lipid-based carrier to control the post-surgical infection. In this study, CPX was formulated as ophthalmic liposomal drops. Two different phospholipids in different ratios were utilized, including phosphatidylcholine (PC) and dimyrestoyl phosphatidylcholine (DMPC). The physiochemical properties of the prepared ophthalmic liposomes were evaluated in terms of particle size, entrapment efficiency, polydispersity index, zeta potential, and cumulative CPX in-vitro release. In addition, the effect of sonication time on particle size and entrapment efficiency of CPX ophthalmic drops was also evaluated. The results revealed that most of the prepared formulations showed particle size in nanometer size range (460–1047 nm) and entrapment efficiency ranging from 36.4–44.7%. The antibacterial activity and minimum inhibitory concentration (MIC) were investigated. Ex vivo antimicrobial effect of promising formulations was carried out against the most common causes of endophthalmitis microorganisms. The pharmacokinetics of the prepared ophthalmic drops were tested in rabbit aqueous humor and compared with commercial CPX ophthalmic drops (Ciloxan®). Observed bacterial suppression was detected in rabbit’s eyes conjunctivitis with an optimized formulation A3 compared with the commercial ophthalmic drops. CPX concentration in the aqueous humor was above MIC against tested bacterial strains. The in vivo data revealed that the tested CPX drops showed superiority over the commercial ones with respect to peak aqueous humor concentration, time to reach peak aqueous humor concentration, elimination rate constant, half-life, and relative bioavailability. Based on these results, it was concluded that the prepared ophthalmic formulations significantly enhanced CPX bioavailability compared with the commercial one. Full article
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15 pages, 977 KiB  
Article
Hepatoprotective Effects of Bioflavonoid Luteolin Using Self-Nanoemulsifying Drug Delivery System
by Faiyaz Shakeel, Moad M. Alamer, Prawez Alam, Abdullah Alshetaili, Nazrul Haq, Fars K. Alanazi, Sultan Alshehri, Mohammed M. Ghoneim and Ibrahim A. Alsarra
Molecules 2021, 26(24), 7497; https://doi.org/10.3390/molecules26247497 - 11 Dec 2021
Cited by 20 | Viewed by 2913
Abstract
Luteolin (LUT) is a natural pharmaceutical compound that is weakly water soluble and has low bioavailability when taken orally. As a result, the goal of this research was to create self-nanoemulsifying drug delivery systems (SNEDDS) for LUT in an attempt to improve its [...] Read more.
Luteolin (LUT) is a natural pharmaceutical compound that is weakly water soluble and has low bioavailability when taken orally. As a result, the goal of this research was to create self-nanoemulsifying drug delivery systems (SNEDDS) for LUT in an attempt to improve its in vitro dissolution and hepatoprotective effects, resulting in increased oral bioavailability. Using the aqueous phase titration approach and the creation of pseudo-ternary phase diagrams with Capryol-PGMC (oil phase), Tween-80 (surfactant), and Transcutol-HP (co-emulsifier), various SNEDDS of LUT were generated. SNEDDS were assessed for droplet size, polydispersity index (PDI), zeta potential (ZP), refractive index (RI), and percent of transmittance (percent T) after undergoing several thermodynamic stability and self-nanoemulsification experiments. When compared to LUT suspension, the developed SNEDDS revealed considerable LUT release from all SNEDDS. Droplet size was 40 nm, PDI was <0.3, ZP was −30.58 mV, RI was 1.40, percent T was >98 percent, and drug release profile was >96 percent in optimized SNEDDS of LUT. For in vivo hepatoprotective testing in rats, optimized SNEDDS was chosen. When compared to LUT suspension, hepatoprotective tests showed that optimized LUT SNEDDS had a substantial hepatoprotective impact. The findings of this investigation suggested that SNEDDS could improve bioflavonoid LUT dissolution rate and therapeutic efficacy. Full article
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Review

Jump to: Editorial, Research

19 pages, 1575 KiB  
Review
Quality by Design Approach in Liposomal Formulations: Robust Product Development
by Walhan Alshaer, Hamdi Nsairat, Zainab Lafi, Omar M. Hourani, Abdulfattah Al-Kadash, Ezaldeen Esawi and Alaaldin M. Alkilany
Molecules 2023, 28(1), 10; https://doi.org/10.3390/molecules28010010 - 20 Dec 2022
Cited by 15 | Viewed by 6107
Abstract
Nanomedicine is an emerging field with continuous growth and differentiation. Liposomal formulations are a major platform in nanomedicine, with more than fifteen FDA-approved liposomal products in the market. However, as is the case for other types of nanoparticle-based delivery systems, liposomal formulations and [...] Read more.
Nanomedicine is an emerging field with continuous growth and differentiation. Liposomal formulations are a major platform in nanomedicine, with more than fifteen FDA-approved liposomal products in the market. However, as is the case for other types of nanoparticle-based delivery systems, liposomal formulations and manufacturing is intrinsically complex and associated with a set of dependent and independent variables, rendering experiential optimization a tedious process in general. Quality by design (QbD) is a powerful approach that can be applied in such complex systems to facilitate product development and ensure reproducible manufacturing processes, which are an essential pre-requisite for efficient and safe therapeutics. Input variables (related to materials, processes and experiment design) and the quality attributes for the final liposomal product should follow a systematic and planned experimental design to identify critical variables and optimal formulations/processes, where these elements are subjected to risk assessment. This review discusses the current practices that employ QbD in developing liposomal-based nano-pharmaceuticals. Full article
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21 pages, 950 KiB  
Review
Exploring the Potential of Natural Product-Based Nanomedicine for Maintaining Oral Health
by Rajeev Kumar, Mohd A. Mirza, Punnoth Poonkuzhi Naseef, Mohamed Saheer Kuruniyan, Foziyah Zakir and Geeta Aggarwal
Molecules 2022, 27(5), 1725; https://doi.org/10.3390/molecules27051725 - 7 Mar 2022
Cited by 17 | Viewed by 5408
Abstract
Oral diseases pose a major threat to public health across the globe. Diseases such as dental caries, periodontitis, gingivitis, halitosis, and oral cancer affect people of all age groups. Moreover, unhealthy diet practices and the presence of comorbidities aggravate the problem even further. [...] Read more.
Oral diseases pose a major threat to public health across the globe. Diseases such as dental caries, periodontitis, gingivitis, halitosis, and oral cancer affect people of all age groups. Moreover, unhealthy diet practices and the presence of comorbidities aggravate the problem even further. Traditional practices such as the use of miswak for oral hygiene and cloves for toothache have been used for a long time. The present review exhaustively explains the potential of natural products obtained from different sources for the prevention and treatment of dental diseases. Additionally, natural medicine has shown activity in preventing bacterial biofilm resistance and can be one of the major forerunners in the treatment of oral infections. However, in spite of the enormous potential, it is a less explored area due to many setbacks, such as unfavorable physicochemical and pharmacokinetic properties. Nanotechnology has led to many advances in the dental industry, with various applications ranging from maintenance to restoration. However, can nanotechnology help in enhancing the safety and efficacy of natural products? The present review discusses these issues in detail. Full article
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26 pages, 3482 KiB  
Review
Smart Nanocarriers as an Emerging Platform for Cancer Therapy: A Review
by Madhuchandra Kenchegowda, Mohamed Rahamathulla, Umme Hani, Mohammed Y. Begum, Sagar Guruswamy, Riyaz Ali M. Osmani, Mysore P. Gowrav, Sultan Alshehri, Mohammed M. Ghoneim, Areej Alshlowi and Devegowda V. Gowda
Molecules 2022, 27(1), 146; https://doi.org/10.3390/molecules27010146 - 27 Dec 2021
Cited by 79 | Viewed by 7606
Abstract
Cancer is a group of disorders characterized by uncontrolled cell growth that affects around 11 million people each year globally. Nanocarrier-based systems are extensively used in cancer imaging, diagnostics as well as therapeutics; owing to their promising features and potential to augment therapeutic [...] Read more.
Cancer is a group of disorders characterized by uncontrolled cell growth that affects around 11 million people each year globally. Nanocarrier-based systems are extensively used in cancer imaging, diagnostics as well as therapeutics; owing to their promising features and potential to augment therapeutic efficacy. The focal point of research remains to develop new-fangled smart nanocarriers that can selectively respond to cancer-specific conditions and deliver medications to target cells efficiently. Nanocarriers deliver loaded therapeutic cargos to the tumour site either in a passive or active mode, with the least drug elimination from the drug delivery systems. This review chiefly focuses on current advances allied to smart nanocarriers such as dendrimers, liposomes, mesoporous silica nanoparticles, quantum dots, micelles, superparamagnetic iron-oxide nanoparticles, gold nanoparticles and carbon nanotubes, to list a few. Exhaustive discussion on crucial topics like drug targeting, surface decorated smart-nanocarriers and stimuli-responsive cancer nanotherapeutics responding to temperature, enzyme, pH and redox stimuli have been covered. Full article
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