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Pharmaceutics
Special Issues
Micro- and Nano-Emulsions as Drug Delivery Systems
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Micro- and Nano-Emulsions as Drug Delivery Systems

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: closed (31 March 2024) | Viewed by 4958

Special Issue Editors

Prof. Dr. Han-Joo Maeng

E-Mail Website
Guest Editor
College of Pharmacy, Gachon University, 191 Hambakmoe-ro, Yeonsu-gu, Incheon 21936, Republic of Korea
Interests: pharmacokinetics; biopharmaceutics; absorption; drug transporters; metabolic enzymes; drug delivery; nanoparticles
Special Issues, Collections and Topics in MDPI journals
Dr. Alam Zeb

E-Mail Website
Guest Editor
Riphah Institute of Pharmaceutical Sciences, Riphah International University, Islamabad 44000, Pakistan
Interests: drug delivery; nanomedicine; lipid nanoparticles; liposomes; emulsions; hydrogels

Special Issue Information

Dear Colleagues,

We are inviting manuscripts for publication in a Special Issue of Pharmaceutics entitled “Micro- and Nano-Emulsions as Drug Delivery Systems”. Emulsions are biphasic liquid–liquid systems where one liquid is dispersed (i.e., internal phase) as small droplets in another liquid (i.e., external phase). Micro- and nano-emulsions are particular types of thermodynamically stable emulsions with droplets sized down to the nano-metric range. In recent years, micro- and nano-emulsions have received profound interest from the pharmaceutical, food, and cosmetic industries as they are capable to modify and improve the physicochemical properties and efficacy of their payload. In addition, they can accommodate drugs with a polar and nonpolar nature, solubilize poorly water-soluble drugs, and offer opportunities to produce stimulus responsive nanomedicines. Self-micro- and self-nano-emulsifying drug delivery systems (SMEDDS and SNEDDS) are also considered special types of emulsions consisting of oil and surfactant with the occasional addition of cosolvents and cosurfactants. These monophasic systems readily produce emulsion when exposed to mild agitation of fluid in the gastrointestinal tract (GIT). Their use to enhance aqueous solubility, dissolution, and oral bioavailability of poorly water-soluble drugs such as BCS class II drugs is well-known. In addition, these emulsions can be applied for nasal and transdermal delivery. This Special Issue aims to highlight recent advances, trends, and applications of micro- and nano-emulsions. Keeping in view their tremendous potential in drug delivery, we welcome researchers to submit research and review articles addressing novel production techniques, formulation strategies, and applications of micro- and nano-emulsions.

Prof. Dr. Han-Joo Maeng
Dr. Alam Zeb
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

  • micro-emulsions
  • nano-emulsions 
  • self-micro-emulsifying drug delivery systems (SMEDDS) 
  • self-nano-emulsifying drug delivery systems (SNEDDS) 
  • poorly water-soluble drugs 
  • dissolution 
  • oral bioavailability 
  • pharmacokinetics

Published Papers (3 papers)

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Research

20 pages, 4500 KiB  
Article
Formulation and Evaluation of a Self-Microemulsifying Drug Delivery System of Raloxifene with Improved Solubility and Oral Bioavailability
by Muhammad Mohsin Ansari, Dang-Khoa Vo, Ho-Ik Choi, Jeong-Su Ryu, Yumi Bae, Nadeem Irfan Bukhari, Alam Zeb, Jin-Ki Kim and Han-Joo Maeng
Pharmaceutics 2023, 15(8), 2073; https://doi.org/10.3390/pharmaceutics15082073 - 02 Aug 2023
Cited by 1 | Viewed by 1536
Abstract
Poor aqueous solubility and dissolution limit the oral bioavailability of Biopharmaceutics Classification System (BCS) class II drugs. In this study, we aimed to improve the aqueous solubility and oral bioavailability of raloxifene hydrochloride (RLX), a BCS class II drug, using a self-microemulsifying drug [...] Read more.
Poor aqueous solubility and dissolution limit the oral bioavailability of Biopharmaceutics Classification System (BCS) class II drugs. In this study, we aimed to improve the aqueous solubility and oral bioavailability of raloxifene hydrochloride (RLX), a BCS class II drug, using a self-microemulsifying drug delivery system (SMEDDS). Based on the solubilities of RLX, Capryol 90, Tween 80/Labrasol ALF, and polyethylene glycol 400 (PEG-400) were selected as the oil, surfactant mixture, and cosurfactant, respectively. Pseudo-ternary phase diagrams were constructed to determine the optimal composition (Capryol 90/Tween 80/Labrasol ALF/PEG-400 in 150/478.1/159.4/212.5 volume ratio) for RLX-SMEDDS with a small droplet size (147.1 nm) and stable microemulsification (PDI: 0.227). Differential scanning calorimetry and powder X-ray diffraction of lyophilized RLX-SMEDDS revealed the loss of crystallinity, suggesting a molecularly dissolved or amorphous state of RLX in the SMEDDS formulation. Moreover, RLX-SMEDDS exhibited significantly higher saturation solubility and dissolution rate in water, simulated gastric fluid (pH 1.2), and simulated intestinal fluid (pH 6.8) than RLX powder. Additionally, oral administration of RLX-SMEDDS to female rats resulted in 1.94- and 1.80-fold higher area under the curve and maximum plasma concentration, respectively, than the RLX dispersion. Collectively, our findings suggest SMEDDS is a promising oral formulation to enhance the therapeutic efficacy of RLX. Full article
(This article belongs to the Special Issue Micro- and Nano-Emulsions as Drug Delivery Systems)
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16 pages, 4728 KiB  
Article
Design and Evaluation of Hydrophobic Ion Paired Insulin Loaded Self Micro-Emulsifying Drug Delivery System for Oral Delivery
by Jahanzeb Mudassir, Afsheen Raza, Mahtab Ahmad Khan, Huma Hameed, Gamal A. Shazly, Ali Irfan, Sadia Jafar Rana, Khizar Abbas, Muhammad Sohail Arshad, Sajjad Muhammad and Yousef A. Bin Jardan
Pharmaceutics 2023, 15(7), 1973; https://doi.org/10.3390/pharmaceutics15071973 - 18 Jul 2023
Cited by 3 | Viewed by 1334
Abstract
Despite several novel and innovative approaches, clinical translation of oral insulin delivery into commercially viable treatment is still challenging due to its poor absorption and rapid degradation in GIT. Thus, an insulin-SDS hydrophobic ion pair loaded self-microemulsifying drug delivery system (SMEDDS) was formulated [...] Read more.
Despite several novel and innovative approaches, clinical translation of oral insulin delivery into commercially viable treatment is still challenging due to its poor absorption and rapid degradation in GIT. Thus, an insulin-SDS hydrophobic ion pair loaded self-microemulsifying drug delivery system (SMEDDS) was formulated to exploit the hypoglycemic effects of orally delivered insulin. Insulin was initially hydrophobically ion paired with sodium dodecyl sulphate (SDS) to enhance its lipophilicity. The successful complexation of Insulin-SDS was confirmed by FTIR and surface morphology was evaluated using SEM. Stability of insulin after its release from HIP complex was evaluated using SDS PAGE. Subsequently, Ins-SDS loaded SMEDDS was optimized using two factorial designs. In vitro stability of insulin entrapped in optimized SMEDDS against proteolytic degradation was also assessed. Further, antidiabetic activity of optimized Ins-SDS loaded SMEDDS was evaluated in diabetic rats. Insulin complexed with SDS at 6:1 (SDS/insulin) molar ratio with almost five-fold increased lipophilicity. The SMEDDS was optimized at 10% Labraphil M2125 CS, 70% Cremophore EL, and 20% Transcutol HP with better proteolytic stability and oral antidiabetic activity. An Ins-SDS loaded SMEDDS was successfully optimized. Compared with insulin and Ins-SDS complex, the optimized SMEDDS displayed considerable resistance to GI enzymes. Thus, the SMEDDS showed potential for effective delivery of macromolecular drugs with improved oral bioavailability. Full article
(This article belongs to the Special Issue Micro- and Nano-Emulsions as Drug Delivery Systems)
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13 pages, 1890 KiB  
Article
Development and Evaluation of Self-Microemulsifying Drug Delivery System for Improving Oral Absorption of Poorly Water-Soluble Olaparib
by Yong-Han Kim, Seong-Bo Kim, Se-Hee Choi, Thi-Thao-Linh Nguyen, Sung-Hoon Ahn, Kyung-Sun Moon, Kwan-Hyung Cho, Tae-Yong Sim, Eun-Ji Heo, Sung Tae Kim, Hyun-Suk Jung, Jun-Pil Jee, Han-Gon Choi and Dong-Jin Jang
Pharmaceutics 2023, 15(6), 1669; https://doi.org/10.3390/pharmaceutics15061669 - 07 Jun 2023
Viewed by 1587
Abstract
The purpose of this study is to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) to improve the oral absorption of poorly water-soluble olaparib. Through the solubility test of olaparib in various oils, surfactants and co-surfactants, pharmaceutical excipients were selected. Self-emulsifying regions [...] Read more.
The purpose of this study is to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) to improve the oral absorption of poorly water-soluble olaparib. Through the solubility test of olaparib in various oils, surfactants and co-surfactants, pharmaceutical excipients were selected. Self-emulsifying regions were identified by mixing the selected materials at various ratios, and a pseudoternary phase diagram was constructed by synthesizing these results. The various physicochemical properties of microemulsion incorporating olaparib were confirmed by investigating the morphology, particle size, zeta potential, drug content and stability. In addition, the improved dissolution and absorption of olaparib were also confirmed through a dissolution test and a pharmacokinetic study. An optimal microemulsion was generated in the formulation of Capmul® MCM 10%, Labrasol® 80% and PEG 400 10%. The fabricated microemulsions were well-dispersed in aqueous solutions, and it was also confirmed that they were maintained well without any problems of physical or chemical stability. The dissolution profiles of olaparib were significantly improved compared to the value of powder. Associated with the high dissolutions of olaparib, the pharmacokinetic parameters were also greatly improved. Taken together with the results mentioned above, the microemulsion could be an effective tool as a formulation for olaparib and other similar drugs. Full article
(This article belongs to the Special Issue Micro- and Nano-Emulsions as Drug Delivery Systems)
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