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Pharmaceutics
Special Issues
Microemulsion Utility in Pharmaceuticals
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Microemulsion Utility in Pharmaceuticals

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

Deadline for manuscript submissions: closed (20 December 2024) | Viewed by 11550

Special Issue Editors

Dr. Tao Yi

E-Mail Website
Guest Editor
Faculty of Health Sciences and Sports, Macao Polytechnic University, Macau, China
Interests: drug delivery; nanocrystals; emulsions; nanoparticles
Special Issues, Collections and Topics in MDPI journals
Dr. Jifen Zhang

E-Mail Website
Guest Editor
College of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China
Interests: oral delivery of poorly water-soluble drugs; nanocrystals
Dr. Yi Lu

E-Mail Website
Guest Editor
Key Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, China
Interests: drug delivery; micro/nanoparticles
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are pleased to invite you to submit an article to this Special Issue, entitled “Microemulsion Utility in Pharmaceuticals”. Microemulsions and nanoemulsions are lipid-based liquid systems of water, oil, and stabilizers. Their unique structures and properties endow them with good stability, excellent biocompatibility, rich tunability, and wide applicability. Micro/nanoemulsions have shown great application results and increasing potential in various fields of pharmaceuticals, especially in drug delivery.

This Special Issue aims to provide a forum to promote the development and biomedical applications of micro/nanoemulsions. Original research articles and reviews are welcome. Potential topics include the following: novel stabilizers, types, and preparations of micro/nanoemulsions; mechanisms and factors governing the formation and stability of micro/nanoemulsions; achievements of micro/nanoemulsions in terms of enhanced drug delivery via various routes, e.g., oral, dermal, pulmonary, and parenteral administration; the in vivo fates of micro/nanoemulsions and factors affecting their fates; clinical dosage forms; and quality control. Other submissions that facilitate the development of micro/nanoemulsions are also welcome.

Dr. Tao Yi
Dr. Jifen Zhang
Dr. Yi Lu
Guest Editors

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. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • microemulsions
  • nanoemulsions
  • drug delivery
  • preparation
  • stability
  • characterization
  • biomedical applications
  • bioavailability
  • permeability
  • controlled release
  • in vivo fate

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Published Papers (4 papers)

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Research

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15 pages, 2539 KiB  
Article
Production of Hydrophobic Microparticles at Safe-To-Inject Sizes for Intravascular Administration
by Francisca L. Gomes, Francisco Conceição, Liliana Moreira Teixeira, Jeroen Leijten and Pascal Jonkheijm
Pharmaceutics 2025, 17(1), 64; https://doi.org/10.3390/pharmaceutics17010064 - 6 Jan 2025
Viewed by 840
Abstract
Background/Objectives: Hydrophobic microparticles are one of the most versatile structures in drug delivery and tissue engineering. These constructs offer a protective environment for hydrophobic or water-sensitive compounds (e.g., drugs, peroxides), providing an optimal solution for numerous biomedical purposes, such as drug delivery or [...] Read more.
Background/Objectives: Hydrophobic microparticles are one of the most versatile structures in drug delivery and tissue engineering. These constructs offer a protective environment for hydrophobic or water-sensitive compounds (e.g., drugs, peroxides), providing an optimal solution for numerous biomedical purposes, such as drug delivery or oxygen therapeutics. The intravascular administration of hydrophobic microparticles requires a safe-to-flow particle profile, which typically corresponds to a maximum size of 5 µm—the generally accepted diameter for the thinnest blood vessels in humans. However, the production of hydrophobic microparticles below this size range remains largely unexplored. In this work, we investigate the fabrication of hydrophobic microparticles at safe-to-inject and safe-to-flow sizes (<5 µm) for intravascular administration. Methods: Polycaprolactone microparticles (PCL MPs) are produced using a double-emulsification method with tip ultrasonication, for which various production parameters (PCL molecular weight, PCL concentration, type of stabilizer, and filtration) are optimized to obtain particles at sizes below 5 µm. Results: We achieve a PCL MP size distribution of 99.8% below this size limit, and prove that these particles can flow without obstruction through a microfluidic model emulating a thin human blood capillary (4.1 µm × 3.0 µm width × heigh). Conclusions: Overall, we demonstrate that hydrophobic microparticles can be fabricated at safe-to-flow sizes using a simple and scalable setup, paving the way towards their applicability as new intravascular injectables. Full article
(This article belongs to the Special Issue Microemulsion Utility in Pharmaceuticals)
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14 pages, 3474 KiB  
Article
Triple-Emulsion-Based Antibubbles: A Step Forward in Fabricating Novel Multi-Drug Delivery Systems
by Rabia Zia, Albert T. Poortinga, Akmal Nazir, Salahdein Aburuz and Cornelus F. van Nostrum
Pharmaceutics 2023, 15(12), 2757; https://doi.org/10.3390/pharmaceutics15122757 - 12 Dec 2023
Cited by 4 | Viewed by 1658
Abstract
Developing carriers capable of efficiently transporting both hydrophilic and lipophilic payloads is a captivating focus within the pharmaceutical and drug delivery research domain. Antibubbles, constituting an innovative encapsulation system designed for drug delivery purposes, have garnered scientific interest thanks to their distinctive water-in-air-in-water [...] Read more.
Developing carriers capable of efficiently transporting both hydrophilic and lipophilic payloads is a captivating focus within the pharmaceutical and drug delivery research domain. Antibubbles, constituting an innovative encapsulation system designed for drug delivery purposes, have garnered scientific interest thanks to their distinctive water-in-air-in-water (W1/A/W2) structure. However, in contrast to their precursor, i.e., nanoparticle-stabilized W1/O/W2 double emulsion, traditional antibubbles lack the ability to accommodate a lipophilic payload, as the intermediary (volatile) oil layer of the emulsion is replaced by air during the antibubble fabrication process. Therefore, here, we report the fabrication of triple-emulsion-based antibubbles (O1/W1/A/W2), in which the inner aqueous phase was loaded with a nanoemulsion stabilized by various proteins, including whey, soy, or pea protein isolates. As model drugs, we employed the dyes Nile red in the oil phase and methylene blue in the aqueous phase. The produced antibubbles were characterized regarding their size distribution, entrapment efficiency, and stability. The produced antibubbles demonstrated substantial entrapment efficiencies for both lipophilic (ranging from 80% to 90%) and hydrophilic (ranging from 70% to 82%) components while also exhibiting an appreciable degree of stability during an extended rehydration period of two weeks. The observed variations among different antibubble variants were primarily attributed to differences in protein concentration rather than the type of protein used. Full article
(This article belongs to the Special Issue Microemulsion Utility in Pharmaceuticals)
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14 pages, 4553 KiB  
Article
Pickering Emulsions Enhance Oral Bioavailability of Curcumin Nanocrystals: The Effect of Oil Types
by Yuze Sheng, Qin Yu, Yanping Huang, Quangang Zhu, Zhongjian Chen, Wei Wu, Tao Yi and Yi Lu
Pharmaceutics 2023, 15(5), 1341; https://doi.org/10.3390/pharmaceutics15051341 - 26 Apr 2023
Cited by 8 | Viewed by 2319
Abstract
Nanocrystals (NCs) have the potential to enhance the oral bioavailability of Class IV drugs in the Biopharmaceutical Classification System (BCS) due to the absorption of the intact crystals. The performance is compromised by the dissolution of NCs. Drug NCs have recently been adopted [...] Read more.
Nanocrystals (NCs) have the potential to enhance the oral bioavailability of Class IV drugs in the Biopharmaceutical Classification System (BCS) due to the absorption of the intact crystals. The performance is compromised by the dissolution of NCs. Drug NCs have recently been adopted as solid emulsifiers to prepare nanocrystal self-stabilized Pickering emulsions (NCSSPEs). They are advantageous in high drug loading and low side effects due to the specific drug loading mode and the absence of chemical surfactants. More importantly, NCSSPEs may further enhance the oral bioavailability of drug NCs by impeding their dissolution. This is especially true for BCS IV drugs. In this study, curcumin (CUR), a typical BCS IV drug, was adopted to prepare CUR-NCs stabilized Pickering emulsions using either indigestible (isopropyl palmitate, IPP) or digestible (soybean oil, SO) oils, i.e., IPP-PEs and SO-PEs. The optimized formulations were spheric with CUR-NCs adsorbed on the water/oil interface. The CUR concentration in the formulation reached 20 mg/mL, which was far beyond the solubility of CUR in IPP (158.06 ± 3.44 μg/g) or SO (124.19 ± 2.40 μg/g). Moreover, the Pickering emulsions enhanced the oral bioavailability of CUR-NCs, being 172.85% for IPP-PEs and 152.07% for SO-PEs. The digestibility of the oil phase affected the amounts of CUR-NCs that remained intact in lipolysis and, thus, the oral bioavailability. In conclusion, converting NCs into Pickering emulsions provides a novel strategy to enhance the oral bioavailability of CUR and BCS IV drugs. Full article
(This article belongs to the Special Issue Microemulsion Utility in Pharmaceuticals)
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Review

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33 pages, 2920 KiB  
Review
Self-Emulsifying Drug Delivery Systems (SEDDS): Transition from Liquid to Solid—A Comprehensive Review of Formulation, Characterization, Applications, and Future Trends
by Prateek Uttreja, Indrajeet Karnik, Ahmed Adel Ali Youssef, Nagarjuna Narala, Rasha M. Elkanayati, Srikanth Baisa, Nouf D. Alshammari, Srikanth Banda, Sateesh Kumar Vemula and Michael A. Repka
Pharmaceutics 2025, 17(1), 63; https://doi.org/10.3390/pharmaceutics17010063 - 5 Jan 2025
Cited by 4 | Viewed by 5269
Abstract
Self-emulsifying drug delivery systems (SEDDS) represent an innovative approach to improving the solubility and bioavailability of poorly water-soluble drugs, addressing significant challenges associated with oral drug delivery. This review highlights the advancements and applications of SEDDS, including their transition from liquid to solid [...] Read more.
Self-emulsifying drug delivery systems (SEDDS) represent an innovative approach to improving the solubility and bioavailability of poorly water-soluble drugs, addressing significant challenges associated with oral drug delivery. This review highlights the advancements and applications of SEDDS, including their transition from liquid to solid forms, while addressing the formulation strategies, characterization techniques, and future prospects in pharmaceutical sciences. The review systematically analyzes existing studies on SEDDS, focusing on their classification into liquid and solid forms and their preparation methods, including spray drying, hot-melt extrusion, and adsorption onto carriers. Characterization techniques such as droplet size analysis, dissolution studies, and solid-state evaluations are detailed. Additionally, emerging trends, including 3D printing, hybrid systems, and supersaturable SEDDS (Su-SEDDS), are explored. Liquid SEDDS (L-SEDDS) enhance drug solubility and absorption by forming emulsions upon contact with gastrointestinal fluids. However, they suffer from stability and leakage issues. Transitioning to solid SEDDS (S-SEDDS) has resolved these limitations, offering enhanced stability, scalability, and patient compliance. Innovations such as personalized 3D-printed SEDDS, biologics delivery, and targeted systems demonstrate their potential for diverse therapeutic applications. Computational modeling and in silico approaches further accelerate formulation optimization. SEDDS have revolutionized drug delivery by improving bioavailability and enabling precise, patient-centric therapies. While challenges such as scalability and excipient toxicity persist, emerging technologies and multidisciplinary collaborations are paving the way for next-generation SEDDS. Their adaptability and potential for personalized medicine solidify their role as a cornerstone in modern pharmaceutical development. Full article
(This article belongs to the Special Issue Microemulsion Utility in Pharmaceuticals)
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