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Dosage Form Formulation Technologies for Improving Bioavailability

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A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: closed (10 November 2023) | Viewed by 29284

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Dr. Gábor Vasvári

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Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, H-4032 Debrecen, Hungary
Interests: novel drug delivery; nano- and microformulations; stability investigation of drug delivery formulations; investigation of solubility, solubility enhancing technology

Dr. Ádám Haimhoffer

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Guest Editor

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei Körút 98, H-4032 Debrecen, Hungary
Interests: gastroretention; dosage form design; in vivo bioavability; cyclodextrin; cyclodextrin-polymer

Special Issue Information

Dear Colleagues,

The challenges of drug development could be extremely tough, high risk of failure or non-approval competes with the great benefits following the successful marketing authorization of a new molecular entities. Therefore, the more effective formulation in dosage form design is vital to overcome the possible disadvantageous physicochemical or biopharmaceutical properties of an approved API. Improving the oral, transdermal, or parenteral bioavailability relying on rational dosage form design or redesign, even after years of the market launch would increase therapeutic efficacies or patient compliance and lower the severity and the occurrence of unwanted side-effects. Innovative techniques, technological applications together with recently developed excipients would open the doors to the global markets for more patient-friendly products.

This Special Issue welcomes original research papers especially, but not limited to cooperative works between academia and pharmaceutical companies, where reformulations or original dosage form design were performed. Papers or reviews including the principles of Quality by Design to improve the bioavailability of drug belonging to BCS Classes of II or IV are warmly encouraged for submission. We are looking for manuscripts that optimize the innovative technology by the design of experiments as well. Non-pharma institutes or departments and their innovative research projects are also invited to contribute this Special Issue, if their novel and original results could be adapted to dosage form formulation or production.

Dr. Gábor Vasvári
Dr. Ádám Haimhoffer
Guest Editors

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Keywords

innovative formulations
drug release optimization
pharmaceutical dosage form
quality by design
design of experiments
novel technologies
solubility enhancement
orphan drug

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Published Papers (12 papers)

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Research

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16 pages, 7043 KiB

Open AccessArticle

Formulation and Evaluation of Insulin-Loaded Sodium-Alginate Microparticles for Oral Administration

by Ildikó Bácskay, Boglárka Papp, Péter Pártos, István Budai, Ágota Pető, Pálma Fehér, Zoltán Ujhelyi and Dóra Kósa

Pharmaceutics 2024, 16(1), 46; https://doi.org/10.3390/pharmaceutics16010046 - 28 Dec 2023

Viewed by 1545

Abstract

The development of oral insulin drug delivery systems is still an ongoing challenge for pharmaceutical technology researchers, as the formulation process has to overcome a number of obstacles due to the adverse characteristics of peptides. The aim of this study was to formulate different sodium-alginate microparticles as a possible method for oral insulin administration. In our previous studies, the method has been successfully optimized using a small model peptide. The incorporation of insulin into alginate carriers containing nonionic surfactants has not been described yet. In order to enhance the absorption of insulin through biological barriers, Labrasol ALF and Labrafil M 2125 CS were selected as permeation-enhancing excipients. They were applied at a concentration of 0.10% (v/v%), along with various combinations of the two, to increase oral bioavailability. Encapsulation efficiency showed sufficient drug incorporation, as it resulted in over 80% in each composition. In vitro dissolution and enzymatic stability test results proved that, as a pH-responsive polymer, alginate bead swelling and drug release occur at higher pH, thus protecting insulin against the harsh environment of the gastrointestinal tract. The remaining insulin content was 66% due to SIF degradation after 120 min. Permeability experiments revealed the impact of permeation enhancers and natural polymers on drug absorption, as they enhanced drug transport significantly through Caco-2 cells in the case of alginate microparticle formulations, as opposed to the control insulin solution. These results suggest that these formulations are able to improve the oral bioavailability of insulin. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

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18 pages, 10897 KiB

Open AccessArticle

Formulation and Evaluation of Transdermal Patches Containing BGP-15

by Ildikó Bácskay, Zsolt Hosszú, István Budai, Zoltán Ujhelyi, Pálma Fehér, Dóra Kósa, Ádám Haimhoffer and Ágota Pető

Pharmaceutics 2024, 16(1), 36; https://doi.org/10.3390/pharmaceutics16010036 - 27 Dec 2023

Cited by 1 | Viewed by 3744

Abstract

BGP-15 is an active ingredient with many advantages, e.g., beneficial cardiovascular and anti-inflammatory effects. The transdermal administration of BGP-15 has great potential, which has not been investigated yet, despite the fact that it is a non-invasive and safe form of treatment. The aim of our study was to formulate transdermal patches containing BGP-15 and optimize the production with the Box–Behnken design of experiment. The most optimal formulation was further combined with penetration enhancers to improve bioavailability of the active ingredient, and the in vitro drug release and in vitro permeation of BGP-15 from the patches were investigated. FTIR spectra of BGP-15, the formulations and the components were also studied. The most optimal formulation based on the tested parameters was dried for 24 h, with 67% polyvinyl alcohol (PVA) content and low ethanol content. The selected penetration enhancer excipients were not cytotoxic on HaCaT cells. The FTIR measurements and SEM photography proved the compatibility of the active substance and the vehicle; BGP-15 was present in the polymer matrix in dissolved form. The bioavailability of BGP-15 was most significantly enhanced by the combination of Transcutol and Labrasol. The in vitro permeation study confirmed that the formulated patches successfully enabled the transdermal administration of BGP-15. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

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18 pages, 4618 KiB

Open AccessArticle

Formulation and Investigation of CK2 Inhibitor-Loaded Alginate Microbeads with Different Excipients

by Boglárka Papp, Marc Le Borgne, Florent Perret, Christelle Marminon, Liza Józsa, Ágota Pető, Dóra Kósa, Lajos Nagy, Sándor Kéki, Zoltán Ujhelyi, Ádám Pallér, István Budai, Ildikó Bácskay and Pálma Fehér

Pharmaceutics 2023, 15(12), 2701; https://doi.org/10.3390/pharmaceutics15122701 - 29 Nov 2023

Cited by 1 | Viewed by 1510

Abstract

The aim of this study was to formulate and characterize CK2 inhibitor-loaded alginate microbeads via the polymerization method. Different excipients were used in the formulation to improve the penetration of an active agent and to stabilize our preparations. Transcutol^® HP was added to the drug–sodium alginate mixture and polyvinylpyrrolidone (PVP) was added to the hardening solution, alone and in combination. To characterize the formulations, mean particle size, scanning electron microscopy analysis, encapsulation efficiency, swelling behavior, an enzymatic stability test and an in vitro dissolution study were performed. The cell viability assay and permeability test were also carried out on the Caco-2 cell line. The anti-oxidant and anti-inflammatory effects of the formulations were finally evaluated. The combination of Transcutol^® HP and PVP in the formulation of sodium alginate microbeads could improve the stability, in vitro permeability, anti-oxidant and anti-inflammatory effects of the CK2 inhibitor. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

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11 pages, 3821 KiB

Open AccessArticle

The Development of Lipid-Based Sorafenib Granules to Enhance the Oral Absorption of Sorafenib

by Jaylen C. Mans and Xiaowei Dong

Pharmaceutics 2023, 15(12), 2691; https://doi.org/10.3390/pharmaceutics15122691 - 28 Nov 2023

Cited by 2 | Viewed by 1310

Abstract

Sorafenib (SFN) is an anticancer multi-kinase inhibitor with great therapeutic potential. However, SFN has low aqueous solubility, which limits its oral absorption. Lipids and surfactants have the potential to improve the solubility of water-insoluble drugs. The aim of this study is thus to develop novel lipid-based SFN granules that can improve the oral absorption of SFN. SFN powder was coated with a stable binary lipid mixture and then absorbed on Aeroperl 300 to form dry SFN granules with 10% drug loading. SFN granules were stable at room temperature for at least three months. Compared to SFN powder, SFN granules significantly increased SFN release in simulated gastric fluid and simulated intestinal fluid with pancreatin. Pharmacokinetics and tissue distribution of SFN granules and SFN powder were measured following oral administration to Sprague Dawley rats. SFN granules significantly increased SFN absorption compared to SFN powder. Overall, the lipid-based SFN granules provide a promising approach to enhancing the oral absorption of SFN. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

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15 pages, 2357 KiB

Open AccessArticle

Enhancing Pharmacokinetics and Pharmacodynamics of Rosuvastatin Calcium through the Development and Optimization of Fast-Dissolving Films

by Ibrahim Ashraf, Pierre A. Hanna, Shadeed Gad, Fathy I. Abd-Allah and Khalid M. El-Say

Pharmaceutics 2023, 15(11), 2640; https://doi.org/10.3390/pharmaceutics15112640 - 19 Nov 2023

Cited by 2 | Viewed by 1957

Abstract

Rosuvastatin (RSV) is a widely used cholesterol-lowering medication, but its limited bioavailability due to its susceptibility to stomach pH and extensive first-pass metabolism poses a significant challenge. A fast-dissolving film (FDF) formulation of RSV was developed, characterized, and compared to the conventional marketed tablet to address this issue. The formulation process involved optimizing the thickness, disintegration time, and folding durability. All formulations were assessed for in vitro disintegration, thickness, folding endurance, in vitro dissolution, weight, and content uniformity. The study’s results revealed that the optimized RSV-FDF displayed a significantly faster time to maximum plasma concentration (t_max) of 2 h, compared to 4 h for the marketed tablet. The maximum plasma concentration (C_max) for the RSV-FDF (1.540 µg/mL ± 0.044) was notably higher than that of the marketed tablet (0.940 µg/mL ± 0.017). Additionally, the pharmacodynamic assessment in male Wistar rats demonstrated that the optimized RSV-FDF exhibited an improved lipid profile, including reduced levels of low-density lipoproteins (LDLs), elevated high-density lipoproteins (HDLs), decreased triglycerides (TGs), and lower very-low-density lipoproteins (VLDLs) compared to the conventional tablet. These findings underscore the potential of RSV-FDFs as a promising alternative to enhance the bioavailability and therapeutic efficacy of rosuvastatin in treating dyslipidemia. The faster onset of action and improved lipid-lowering effects make RSV-FDFs an attractive option for patients requiring efficient cholesterol management. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

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16 pages, 2278 KiB

Open AccessArticle

Computational Amendment of Parenteral In Situ Forming Particulates’ Characteristics: Design of Experiment and PBPK Physiological Modeling

by Nada M. El Hoffy, Ahmed S. Yacoub, Amira M. Ghoneim, Magdy Ibrahim, Hussein O. Ammar and Nermin Eissa

Pharmaceutics 2023, 15(10), 2513; https://doi.org/10.3390/pharmaceutics15102513 - 23 Oct 2023

Viewed by 1555

Abstract

Lipid and/or polymer-based drug conjugates can potentially minimize side effects by increasing drug accumulation at target sites and thus augment patient compliance. Formulation factors can present a potent influence on the characteristics of the obtained systems. The selection of an appropriate solvent with satisfactory rheological properties, miscibility, and biocompatibility is essential to optimize drug release. This work presents a computational study of the effect of the basic formulation factors on the characteristics of the obtained in situ-forming particulates (IFPs) encapsulating a model drug using a 2¹.3¹ full factorial experimental design. The emulsion method was employed for the preparation of lipid and/or polymer-based IFPs. The IFP release profiles and parameters were computed. Additionally, a desirability study was carried out to choose the optimum formulation for further morphological examination, rheological study, and PBPK physiological modeling. Results revealed that the type of particulate forming agent (lipid/polymer) and the incorporation of structure additives like Brij 52 and Eudragit RL can effectively augment the release profile as well as the burst of the drug. The optimized formulation exhibited a pseudoplastic rheological behavior and yielded uniformly spherical-shaped dense particulates with a PS of 573.92 ± 23.5 nm upon injection. Physiological modeling simulation revealed the pioneer pharmacokinetic properties of the optimized formulation compared to the observed data. These results assure the importance of controlling the formulation factors during drug development, the potentiality of the optimized IFPs for the intramuscular delivery of piroxicam, and the reliability of PBPK physiological modeling in predicting the biological performance of new formulations with effective cost management. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

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24 pages, 2019 KiB

Open AccessArticle

Co-Dispersion Delivery Systems with Solubilizing Carriers Improving the Solubility and Permeability of Cannabinoids (Cannabidiol, Cannabidiolic Acid, and Cannabichromene) from Cannabis sativa (Henola Variety) Inflorescences

by Anna Stasiłowicz-Krzemień, Piotr Szulc and Judyta Cielecka-Piontek

Pharmaceutics 2023, 15(9), 2280; https://doi.org/10.3390/pharmaceutics15092280 - 4 Sep 2023

Cited by 6 | Viewed by 2484

Abstract

Cannabinoids: cannabidiol (CBD), cannabidiolic acid (CBDA), and cannabichromene (CBC) are lipophilic compounds with limited water solubility, resulting in challenges related to their bioavailability and therapeutic efficacy upon oral administration. To overcome these limitations, we developed co-dispersion cannabinoid delivery systems with the biopolymer polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (Soluplus) and magnesium aluminometasilicate (Neusilin US2) to improve solubility and permeability. Recognizing the potential therapeutic benefits arising from the entourage effect, we decided to work with an extract instead of isolated cannabinoids. Cannabis sativa inflorescences (Henola variety) with a confirming neuroprotective activity were subjected to dynamic supercritical CO₂ (scCO₂) extraction and next they were combined with carriers (1:1 mass ratio) to prepare the co-dispersion cannabinoid delivery systems (HiE). In vitro dissolution studies were conducted to evaluate the solubility of CBD, CBDA, and CBC in various media (pH 1.2, 6.8, fasted, and fed state simulated intestinal fluid). The HiE-Soluplus delivery systems consistently demonstrated the highest dissolution rate of cannabinoids. Additionally, HiE-Soluplus exhibited the highest permeability coefficients for cannabinoids in gastrointestinal tract conditions than it was during the permeability studies using model PAMPA GIT. All three cannabinoids exhibited promising blood-brain barrier (BBB) permeability (P_app higher than 4.0 × 10⁻⁶ cm/s), suggesting their potential to effectively cross into the central nervous system. The improved solubility and permeability of cannabinoids from the HiE-Soluplus delivery system hold promise for enhancement in their bioavailability. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

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28 pages, 6085 KiB

Open AccessArticle

Development of Robust Tablet Formulations with Enhanced Drug Dissolution Profiles from Centrifugally-Spun Micro-Fibrous Solid Dispersions of Itraconazole, a BCS Class II Drug

by Stefania Marano, Manish Ghimire, Shahrzad Missaghi, Ali Rajabi-Siahboomi, Duncan Q. M. Craig and Susan A. Barker

Pharmaceutics 2023, 15(3), 802; https://doi.org/10.3390/pharmaceutics15030802 - 1 Mar 2023

Cited by 1 | Viewed by 3002

Abstract

Fibre-based oral drug delivery systems are an attractive approach to addressing low drug solubility, although clear strategies for incorporating such systems into viable dosage forms have not yet been demonstrated. The present study extends our previous work on drug-loaded sucrose microfibres produced by centrifugal melt spinning to examine systems with high drug loading and investigates their incorporation into realistic tablet formulations. Itraconazole, a model BCS Class II hydrophobic drug, was incorporated into sucrose microfibres at 10, 20, 30, and 50% w/w. Microfibres were exposed to high relative humidity conditions (25 °C/75% RH) for 30 days to deliberately induce sucrose recrystallisation and collapse of the fibrous structure into powdery particles. The collapsed particles were successfully processed into pharmaceutically acceptable tablets using a dry mixing and direct compression approach. The dissolution advantage of the fresh microfibres was maintained and even enhanced after humidity treatment for drug loadings up to 30% w/w and, importantly, retained after compression into tablets. Variations in excipient content and compression force allowed manipulation of the disintegration rate and drug content of the tablets. This then permitted control of the rate of supersaturation generation, allowing the optimisation of the formulation in terms of its dissolution profile. In conclusion, the microfibre-tablet approach has been shown to be a viable method for formulating poorly soluble BCS Class II drugs with improved dissolution performance. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

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14 pages, 1654 KiB

Open AccessArticle

The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol Pharmacokinetics

by Laura Di Renzo, Antonella Smeriglio, Mariarosaria Ingegneri, Paola Gualtieri and Domenico Trombetta

Pharmaceutics 2023, 15(3), 743; https://doi.org/10.3390/pharmaceutics15030743 - 23 Feb 2023

Cited by 1 | Viewed by 1566

Abstract

Current evidence supports the use of extra virgin olive oil (EVOO) and its minor components such as hydroxytyrosol or 3,4-dihydroxyphenyl ethanol (DOPET), to improve cardiovascular and metabolic health. Nevertheless, more intervention studies in humans are needed because some gaps remain in its bioavailability and metabolism. The aim of this study was to investigate the DOPET pharmacokinetics on 20 healthy volunteers by administering a hard enteric-coated capsule containing 7.5 mg of bioactive compound conveyed in EVOO. The treatment was preceded by a washout period with a polyphenol and an alcohol-free diet. Blood and urine samples were collected at baseline and different time points, and free DOPET and metabolites, as well as sulfo- and glucuro-conjugates, were quantified by LC-DAD-ESI-MS/MS analysis. The plasma concentration versus time profiles of free DOPET was analyzed by a non-compartmental approach, and several pharmacokinetic parameters (C_max, T_max, T_1/2, AUC_{0–440 min}, AUC_0–∞, AUC_t–∞, AUC_{extrap_pred}, C_last and K_el) were calculated. Results showed that DOPET C_max (5.5 ng/mL) was reached after 123 min (T_max), with a T_1/2 of 150.53 min. Comparing the data obtained with the literature, the bioavailability of this bioactive compound is about 2.5 times higher, confirming the hypothesis that the pharmaceutical formulation plays a pivotal role in the bioavailability and pharmacokinetics of hydroxytyrosol. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

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18 pages, 1545 KiB

Open AccessArticle

Thermoresponsive Azithromycin-Loaded Niosome Gel Based on Poloxamer 407 and Hyaluronic Interactions for Periodontitis Treatment

by Kunchorn Kerdmanee, Thawatchai Phaechamud and Sucharat Limsitthichaikoon

Pharmaceutics 2022, 14(10), 2032; https://doi.org/10.3390/pharmaceutics14102032 - 24 Sep 2022

Cited by 11 | Viewed by 2739

Abstract

Azithromycin (AZM) is a potential antimicrobial drug for periodontitis treatment. However, a potential sustained-release system is needed for intra-periodontal pocket delivery. This study focused on the development and evaluation of a thermoresponsive azithromycin-loaded niosome gel (AZG) to search for a desirable formulation for periodontitis treatment. AZG was further developed from an AZM-loaded niosomal formulation by exploiting the advantages of poloxamer 407 (P407) and hyaluronic acid (HA) interactions. The results showed that the addition of HA decreased the gelation temperature and gelation time of AZG. HA was found to increase the viscosity as well as mucoadhesive and tooth-root surface adhesive properties. The AZG solution state was injectable and exhibited pseudoplastic shear-thinning behavior. P407–HA interactions in AZG could contribute to gel strength. AZG showed 72 h of continuous drug release following the Korsmeyer–Peppas model and potentially enhanced drug permeation. The formulations apparently presented more efficient antibacterial activity against major periodontal pathogens than the standard AZM solution. AZM intra-periodontal pocket formulation and the remarkable properties of niosomes exhibited potential characteristics, including ease of administration, bioadhesion to the anatomical structure of the periodontal pocket, and sustained drug release with competent antimicrobial activity, which could be beneficial for periodontitis treatment. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

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Review

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33 pages, 8953 KiB

Open AccessReview

Exploiting Benefits of Vaterite Metastability to Design Degradable Systems for Biomedical Applications

by Yulia Svenskaya and Tatiana Pallaeva

Pharmaceutics 2023, 15(11), 2574; https://doi.org/10.3390/pharmaceutics15112574 - 2 Nov 2023

Cited by 5 | Viewed by 1779

Abstract

The widespread application of calcium carbonate is determined by its high availability in nature and simplicity of synthesis in laboratory conditions. Moreover, calcium carbonate possesses highly attractive physicochemical properties that make it suitable for a wide range of biomedical applications. This review provides a conclusive analysis of the results on using the tunable vaterite metastability in the development of biodegradable drug delivery systems and therapeutic vehicles with a controlled and sustained release of the incorporated cargo. This manuscript highlights the nuances of vaterite recrystallization to non-porous calcite, dissolution at acidic pH, biodegradation at in vivo conditions and control over these processes. This review outlines the main benefits of vaterite instability for the controlled liberation of the encapsulated molecules for the development of biodegradable natural and synthetic polymeric materials for biomedical purposes. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

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25 pages, 1917 KiB

Open AccessReview

Recent Options and Techniques to Assess Improved Bioavailability: In Vitro and Ex Vivo Methods

by Liza Józsa, Dániel Nemes, Ágota Pető, Dóra Kósa, Réka Révész, Ildikó Bácskay, Ádám Haimhoffer and Gábor Vasvári

Pharmaceutics 2023, 15(4), 1146; https://doi.org/10.3390/pharmaceutics15041146 - 4 Apr 2023

Cited by 12 | Viewed by 4662

Abstract

Bioavailability assessment in the development phase of a drug product is vital to reveal the disadvantageous properties of the substance and the possible technological interventions. However, in vivo pharmacokinetic studies provide strong evidence for drug approval applications. Human and animal studies must be designed on the basis of preliminary biorelevant experiments in vitro and ex vivo. In this article, the authors have reviewed the recent methods and techniques from the last decade that are in use for assessing the bioavailability of drug molecules and the effects of technological modifications and drug delivery systems. Four main administration routes were selected: oral, transdermal, ocular, and nasal or inhalation. Three levels of methodologies were screened for each category: in vitro techniques with artificial membranes; cell culture, including monocultures and co-cultures; and finally, experiments where tissue or organ samples were used. Reproducibility, predictability, and level of acceptance by the regulatory organizations are summarized for the readers. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

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