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Pharmaceutical Excipients in Formulation Design and Drug Delivery

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A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: closed (30 July 2024) | Viewed by 20209

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Special Issue Editor

Prof. Dr. Beverley D. Glass

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Guest Editor

PHARMACY, College of Medicine and Dentistry, James Cook University, Douglas, Townsville, QLD 4811, Australia
Interests: photo-stability; in-use drug stability; drug regulation and quality; falsified medicines, formulation and excipients
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Excipients are the therapeutically inactive components of medication formulations that are essential to ensure the stability, solubility, and bioavailability of the dosage form. Excipients were long considered to be safe and inert, however, there has been increasing concerns around the safety of excipients, particularly in highly susceptible patient populations. Neonates are an example of a highly susceptible patient group due to their vastly underdeveloped metabolic and elimination pathways. The limited availability of daily intake guidelines presents additional challenges to researchers attempting to assess the safe levels of excipient exposure. Patients who have dietary allergies, such as lactose intolerance and celiac disease (allergy to gluten), may also be an at-risk group as gluten and lactose are commonly used as excipients. Finally, patients taking multiple medications may also be at risk, as polypharmacy can increase the exposure to excipients and possibly lead to accumulation. The aim of compiling this Special Issue of Pharmaceuticals on the topic of “Pharmaceutical Excipients in Formulation Design and Drug Delivery” is to draw together experts with knowledge in the field of Excipients across this widely diverse area, including chemists, pharmaceutical and regulatory scientists, and clinicians, who are engaged in contemporary pure and applied research to solve the challenges of delivering quality drug dosage forms, which are safe to all populations. Submissions (original papers and reviews) that contribute to understanding and applications of relevance for Pharmaceutical Excipients in Formulation Design and Drug Delivery are welcomed for this Special Issue.

Prof. Dr. Beverley D. Glass
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

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Keywords

formulation
excipients labelling
adverse effects
inactive ingredients
stability
regulation and quality
safety

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Published Papers (9 papers)

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20 pages, 4906 KiB

Open AccessArticle

Comparing Low-Dose Carvedilol Continuous Manufacturing by Solid and Liquid Feeding in Self-Emulsifying Delivery Systems via Hot Melt EXtrusion (SEDEX)

by Ožbej Zupančič, Josip Matić, Aygün Doğan, Alessio Gaggero, Johannes Khinast and Amrit Paudel

Pharmaceuticals 2024, 17(10), 1290; https://doi.org/10.3390/ph17101290 - 28 Sep 2024

Viewed by 778

Abstract

Background/Objectives: This study compared two pilot scale continuous manufacturing methods of solid self-emulsifying drug delivery systems (SEDDSs) via hot melt extrusion (HME). Methods: A model poorly water-soluble drug carvedilol in low dose (0.5–1.0% w/w) was processed in HME either in a conventional powder form or pre-dissolved in the liquid SEDDS. Results: HME yielded a processable final product with up to 20% w/w SEDDS. Addition of carvedilol powder resulted in a non-homogeneous drug distribution in the extrudates, whereas a homogeneous drug distribution was observed in pre-dissolved carvedilol. SEDDSs were shown to have a plasticizing effect, reducing the HME process torque up to 50%. Compatibility between excipients and carvedilol in the studied ratios after HME was confirmed via DSC and WAXS, demonstrating their amorphous form. Solid SEDDSs with Kollidon^® VA64 self-emulsified in aqueous medium within 15 min with mean droplet sizes 150–200 nm and were independent of the medium temperature, whereas reconstitution of Soluplus^® took over 60 min and mean droplet size increased 2-fold from 70 nm to 150 nm after temperature increased from 25 °C to 37 °C, indicating emulsion phase inversion at cloud point. Conclusions: In conclusion, using Kollidon^® VA64 and pre-dissolved carvedilol in SEDDS has shown to yield a stabile HME process with a homogenous carvedilol content in the extrudate. Full article

(This article belongs to the Special Issue Pharmaceutical Excipients in Formulation Design and Drug Delivery)

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20 pages, 8504 KiB

Open AccessArticle

Ionic Liquid-Based Grapeseed Oil Emulsion for Enhanced Anti-Wrinkle Treatment

by Bo Yang, Xu Zhang, Liguo Zhang, Jinjin Wu, Wei Wang, Qiaomei Huang, Zhenyuan Wang, Jichuan Zhang, Tongjie Xu, Chengyu Wu and Jiaheng Zhang

Pharmaceuticals 2024, 17(10), 1273; https://doi.org/10.3390/ph17101273 - 26 Sep 2024

Viewed by 622

Abstract

Objectives: To address the poor efficacy and percutaneous penetration of grape seed oil, ionic liquids and nanotechnology were combined to prepare a grape seed oil emulsion. Methods: A novel Menthol-CoQ10 ionic liquid and ionic liquid based grapeseed oil emulsion were prepared and confirmed. Results: The average size of the grapeseed oil emulsion was 218 nm, and its zeta potential was −33.5 mV. The ionic liquid-based grape seed oil emulsion exhibited a transdermal penetration effect 4.63-fold higher than that of ordinary grape seed oil emulsion. Ionic liquid also displayed enhanced efficiency both in vitro and in vivo. It significantly inhibited the production of DPPH free radicals and tyrosinase, inhibited melanin and matrix metalloproteinase-1 (MMP-1) produced by cells, and promoted type I collagen expression in fibroblasts. After 28 days of continuous use, the grapeseed oil emulsion improved the water content of the stratum corneum and the rate of transepidermal water loss, enhanced the firmness and elasticity of the skin, and significantly improved the total number and length of under-eye lines, tail lines, nasolabial folds, and marionette lines on the face. Conclusions: Menthol-CoQ10 ionic liquid is a promising functional excipient for both transdermal delivery increase and efficient enhancement. Ionic liquid and nanotechnology for grape seed oil facial mask displayed significantly enhanced efficacy and permeability. Full article

(This article belongs to the Special Issue Pharmaceutical Excipients in Formulation Design and Drug Delivery)

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15 pages, 4225 KiB

Open AccessArticle

Effect of Hydration Forms and Polymer Grades on Theophylline Controlled-Release Tablet: An Assessment and Evaluation

by Molham Sakkal, Mosab Arafat, Priya Yuvaraju, Rami Beiram, Labeeb Ali, Mohammednoor Altarawneh, Abdul Razack Hajamohideen and Salahdein AbuRuz

Pharmaceuticals 2024, 17(3), 271; https://doi.org/10.3390/ph17030271 - 21 Feb 2024

Cited by 1 | Viewed by 1542

Abstract

Background: Drug release from controlled release delivery systems is influenced by various factors, including the polymer’s grade and the drug’s hydration form. This study aimed to investigate the impact of these factors on the controlled release of theophylline (THN). This research compares the monohydrate form found in branded products with the anhydrous form in generic equivalents, each formulated with different polymer grades. Methods: Quality control assessment was conducted alongside in vitro evaluation, complemented by various analytical techniques such as X-ray diffraction (XRD) and scanning electron microscopy (SEM). Additionally, thermal analyses using differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) were employed. Results: Quality control assessments demonstrated that the generic tablets exhibited lower average weight and resistance force compared to the branded ones. In vitro tests revealed that generic tablets released contents within 120 min, compared to 720 min for the branded counterpart. Characterization using XRD and SEM identified disparities in crystallinity and particle distribution between the three samples. Additionally, the thermal analysis indicated consistent endothermic peaks across all samples, albeit with minor variations in heat flow and decomposition temperatures between the two products. Conclusions: This study demonstrated that variations in polymer grade and hydration form significantly impact THN release. Full article

(This article belongs to the Special Issue Pharmaceutical Excipients in Formulation Design and Drug Delivery)

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17 pages, 3834 KiB

Open AccessArticle

Evaluation of Brain Targeting and Antipsychotic Activity of Nasally Administrated Ziprasidone Lipid–Polymer Hybrid Nanocarriers

by Hadel A. Abo El-Enin, Alaa S. Tulbah, Hany W. Darwish, Rania Salama, Ibrahim A. Naguib, Heba A. Yassin and Hend Mohamed Abdel-Bar

Pharmaceuticals 2023, 16(6), 886; https://doi.org/10.3390/ph16060886 - 15 Jun 2023

Cited by 5 | Viewed by 1942

Abstract

The feasibility of using lipid–polymer hybrid (LPH) nanocarriers as a potential platform for the intranasal delivery of ziprasidone (ZP), a second-generation antipsychotic, was explored. Different ZP-loaded LPH composed of a PLGA core and cholesterol-lecithin lipid coat were prepared using a single step nano-precipitation self-assembly technique. Modulation of polymer, lipid and drug amounts, as well as stirring-speed-optimized LPH with a particle size of 97.56 ± 4.55 nm and a ZP entrapment efficiency (EE%) of 97.98 ± 1.22%. The brain deposition and pharmacokinetics studies proved the efficiency of LPH to traverse the blood–brain barrier (BBB) following intranasal delivery with a 3.9-fold increase in targeting efficiency compared to the intravenous (IV) ZP solution with a direct nose-to-brain transport percentage (DTP) of 74.68%. The ZP-LPH showed enhanced antipsychotic activity in terms of animals’ hypermobility over an IV drug solution in schizophrenic rats. The obtained results showed that the fabricated LPH was able to improve ZP brain uptake and proved its antipsychotic efficiency. Full article

(This article belongs to the Special Issue Pharmaceutical Excipients in Formulation Design and Drug Delivery)

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13 pages, 2679 KiB

Open AccessArticle

Lecithin and Chitosan as Building Blocks in Anti-Candida Clotrimazole Nanoparticles

by Lisa Myrseth Hemmingsen, Virginia Panzacchi, Lloyd Mbugua Kangu, Barbara Giordani, Barbara Luppi and Nataša Škalko-Basnet

Pharmaceuticals 2023, 16(6), 790; https://doi.org/10.3390/ph16060790 - 25 May 2023

Cited by 1 | Viewed by 1891

Abstract

The main focus when considering treatment of non-healing and infected wounds is tied to the microbial, particularly bacterial, burden within the wound bed. However, as fungal contributions in these microbial communities become more recognized, the focus needs to be broadened, and the remaining participants in the complex wound microbiome need to be addressed in the development of new treatment strategies. In this study, lecithin/chitosan nanoparticles loaded with clotrimazole were tailored to eradicate one of the most abundant fungi in the wound environment, namely C. albicans. Moreover, this investigation was extended to the building blocks and their organization within the delivery system. In the evaluation of the novel nanoparticles, their compatibility with keratinocytes was confirmed. Furthermore, these biocompatible, biodegradable, and non-toxic carriers comprising clotrimazole (~189 nm, 24 mV) were evaluated for their antifungal activity through both disk diffusion and microdilution methods. It was found that the activity of clotrimazole was fully preserved upon its incorporation into this smart delivery system. These results indicate both that the novel carriers for clotrimazole could serve as a therapeutic alternative in the treatment of fungi-infected wounds and that the building blocks and their organization affect the performance of nanoparticles. Full article

(This article belongs to the Special Issue Pharmaceutical Excipients in Formulation Design and Drug Delivery)

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12 pages, 1840 KiB

Open AccessArticle

Preparation Strategies of the Anti-Mycobacterial Drug Bedaquiline for Intrapulmonary Routes of Administration

by Sara E. Maloney, Ian E. Stewart, Brendan K. Podell, Hadley E. Gary, Jeffrey B. Mecham, Bryan J. Berube, Susan L. Baldwin, Rhea N. Coler and Anthony J. Hickey

Pharmaceuticals 2023, 16(5), 729; https://doi.org/10.3390/ph16050729 - 11 May 2023

Cited by 3 | Viewed by 2231

Abstract

Mycobacterium tuberculosis (M.tb) has infected one-quarter of the world’s population and led to the deaths of 1.6 million individuals in 2021 according to estimates from the World Health Organization. The rise in prevalence of multidrug-resistant and extensively drug-resistant M.tb strains coupled with insufficient therapies to treat such strains has motivated the development of more effective treatments and/or delivery modalities. Bedaquiline, a diarylquinoline antimycobacterial agent, effectively targets mycobacterial ATP synthase but may lead to systemic complications upon oral delivery. Targeted delivery of bedaquiline to the lungs represents an alternative strategy to harness the sterilizing benefits of the drug against M.tb while mitigating off-target side effects. Two pulmonary delivery modalities were developed herein, including dry powder inhalation and liquid instillation. Despite bedaquiline’s poor water solubility, spray drying was performed in predominantly aqueous conditions (≥80%) to avoid a closed-loop, inert system. Aerosols of spray-dried bedaquiline with L-leucine excipient outperformed spray-dried bedaquiline alone, demonstrating superior fine particle fraction metrics (~89% of the emitted dose below <5 µm), suitable for inhalation therapies. Furthermore, the use of a 2-hydroxypropyl-β-cyclodextrin excipient allowed a molecular dispersion of bedaquiline in an aqueous solution for liquid instillation. Both delivery modalities were successfully administered to Hartley guinea pigs for pharmacokinetic analysis and were well-tolerated by the animals. Intrapulmonary liquid delivery of bedaquiline led to adequate serum absorption and appropriate peak serum concentrations of the drug. The liquid formulation was superior in systemic uptake compared to the powder formulation. The predominant route via which M.tb bacilli enter the body is aerosol droplets that are deposited onto airway surfaces. For this reason, we believe that further studies should focus on inhalation or intrapulmonary therapies that target the site of entry and primary site of infection for M.tb. Full article

(This article belongs to the Special Issue Pharmaceutical Excipients in Formulation Design and Drug Delivery)

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14 pages, 2914 KiB

Open AccessArticle

The Use of Calcium Phosphate-Based Starter Pellets for the Preparation of Sprinkle IR MUPS Formulation of Rosuvastatin Calcium

by Krzysztof Cal, Barbara Mikolaszek, Tobias Hess, Markos Papaioannou, Joanna Lenik, Patrycja Ciosek-Skibińska, Helene Wall, Jadwiga Paszkowska, Svitlana Romanova, Grzegorz Garbacz and Daniel Zakowiecki

Pharmaceuticals 2023, 16(2), 242; https://doi.org/10.3390/ph16020242 - 6 Feb 2023

Cited by 1 | Viewed by 3023

Abstract

Sprinkle formulations represent an interesting concept of medicinal products aimed at the steadily growing population of patients suffering from swallowing difficulties (dysphagia). In the present work, immediate-release sprinkle MUPS (multiple-unit pellet system) containing rosuvastatin calcium as a model drug substance was successfully developed. The formulation was prepared by drug layering technique using novel calcium phosphate-based starting pellets (PharSQ^® Spheres CM) of three different particle sizes. The study showed that the developed multiparticulates were characterized by uniform distribution of coating layers thickness, as well as fast dissolution rate (more than 85% of rosuvastatin calcium dissolved within 30 min, as required by the relevant USP/NF monograph). Rosuvastatin calcium, like other statins, has a bitter, unpleasant taste. Investigations conducted with an electronic tongue suggested that the developed formulation achieved the desired taste-masking efficiency. The effect was found to be particle size-dependent, improving as the size of the multiparticulates increased. Full article

(This article belongs to the Special Issue Pharmaceutical Excipients in Formulation Design and Drug Delivery)

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16 pages, 2793 KiB

Open AccessArticle

Design of Novel Tricaprylin-Incorporated Multi-Layered Liposomal System for Skin Delivery of Ascorbic Acid with Improved Chemical Stability

by Myoung Jin Ho, Dong Woo Park and Myung Joo Kang

Pharmaceuticals 2023, 16(1), 121; https://doi.org/10.3390/ph16010121 - 13 Jan 2023

Cited by 5 | Viewed by 2959

Abstract

L-ascorbic acid (Vit C) possesses a variety of dermatological functions in maintaining skin health and anti-aging properties. However, its topical application is challenging owing to its liability to light, oxygen, or heat. Therefore, in this study, a novel liposomal system, including a lipophilic neutral oil named a lipo-oil-some (LOS), was designed to improve the chemical stability and aid the skin absorption of Vit C. The vesicular systems were prepared using the ethanol injection method, employing phosphatidylcholine, cholesterol, dipalmitoyl-sn-glycerol-3-phosphoglycerol, and tricaprylin as neutral oil. The optimized LOS was characterized as follows: shape, multi-layered sphere; size, 981 nm; zeta potential, −58 mV; and Vit C encapsulation efficiency, 35%. The encapsulation of the labile compound into the novel system markedly enhanced photostability, providing over 10% higher Vit C remaining compared to Vit C solution or Vit C-loaded conventional liposome under a light intensity of 20,000 lx. On the other hand, the ex vivo skin permeation and accumulation of Vit C with the LOS system were comparable to those of smaller conventional liposomes (198 nm) in a Franz diffusion cell model mounted with porcine skin. Based on these findings, we concluded that the novel liposomal system could be utilized for skin delivery of Vit C with enhanced chemical stability. Full article

(This article belongs to the Special Issue Pharmaceutical Excipients in Formulation Design and Drug Delivery)

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34 pages, 1269 KiB

Open AccessSystematic Review

Positron Annihilation Lifetime Spectroscopy as a Special Technique for the Solid-State Characterization of Pharmaceutical Excipients, Drug Delivery Systems, and Medical Devices—A Systematic Review

by Mariam Majida Shokoya, Beáta-Mária Benkő, Károly Süvegh, Romána Zelkó and István Sebe

Pharmaceuticals 2023, 16(2), 252; https://doi.org/10.3390/ph16020252 - 7 Feb 2023

Cited by 5 | Viewed by 3482

Abstract

The aims of this systematic review are to explore the possibilities of using the positron annihilation lifetime spectroscopy (PALS) method in the pharmaceutical industry and to examine the application of PALS as a supportive, predictive method during the research process. In addition, the review aims to provide a comprehensive picture of additional medical and pharmaceutical uses, as the application of the PALS test method is limited and not widely known in this sector. We collected the scientific literature of the last 20 years (2002–2022) from several databases (PubMed, Embase, SciFinder-n, and Google Scholar) and evaluated the data gathered in relation to the combination of three directives, namely, the utilization of the PALS method, the testing of solid systems, and their application in the medical and pharmaceutical fields. The application of the PALS method is discussed based on three large groups: substances, drug delivery systems, and medical devices, starting with simpler systems and moving to more complex ones. The results are discussed based on the functionality of the PALS method, via microstructural analysis, the tracking of ageing and microstructural changes during stability testing, the examination of the effects of excipients and external factors, and defect characterization, with a strong emphasis on the benefits of this technique. The review highlights the wide range of possible applications of the PALS method as a non-invasive analytical tool for examining microstructures and monitoring changes; it can be effectively applied in many fields, alone or with complementary testing methods. Full article

(This article belongs to the Special Issue Pharmaceutical Excipients in Formulation Design and Drug Delivery)

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