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Self-Emulsifying Drug Delivery System

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A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (31 December 2020) | Viewed by 36936

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Prof. Dr. Min-Soo Kim

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College of Pharmacy, Pusan National University, 63 Busandaehak-ro, Geumjeong-gu, Busan 46241, Republic of Korea
Interests: sustained and controlled release formulation of drugs; quality by design; formulation and stabilization of emulsion, microemulsion and liposomes; solubilization techniques of poorly water-soluble drugs; polymorphism and cocrystal; coating and pelletization technology; targeted drug delivery system; microspheres and microcapsules; pharmacokinetics and bioequivalent study; drug stability; supercritical fluid technology
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Dear Colleagues,

To date, there has been growing interest in the use of self-emulsifying drug delivery systems (SEDDS) for the development of pharmaceutical dosage forms. SEDDS comprise an optically stable isotropic mixture of a drug, natural or synthetic oils, solid or liquid surfactants, co-surfactants, and/or cosolvents, which generates ultrafine oil droplets upon dilution with an aqueous phase under mild agitation, such as during gastric motility. After self-emulsification in the presence of the aqueous phase, SEDDS provide an ultrafine oil droplet with a large interfacial surface area, which results in the incorporation of poorly water-soluble drugs into fine oil droplets, leading to accelerated drug absorption. In addition, surfactants and cosolvents in the formulations play an important role in improving the transcellular absorption of the drug by increasing the membrane fluidity and permeability.

The aim of this Special Issue of Pharmaceutics is to collect research and review papers on SEDDS applications in the pharmaceutical field. We welcome articles dealing with all aspects of self-emulsifying drug delivery system and invite researchers and drug developers to publish their original research or review articles with expert opinions and perspectives in the area of therapeutics.

Prof. Min-Soo Kim
Guest Editor

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Keywords

self-emulsifying
solubility
dissolution
bioavailability
supersaturation
poorly absorbed drugs
pharmaceutical technology
dosage form

Published Papers (9 papers)

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Research

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16 pages, 2337 KiB

Open AccessArticle

Development of Self-Nanoemulsifying Drug Delivery Systems Containing 4-Allylpyrocatechol for Treatment of Oral Infections Caused by Candida albicans

by Siriporn Okonogi, Pimpak Phumat, Sakornrat Khongkhunthian, Pisaisit Chaijareenont, Thomas Rades and Anette Müllertz

Pharmaceutics 2021, 13(2), 167; https://doi.org/10.3390/pharmaceutics13020167 - 27 Jan 2021

Cited by 8 | Viewed by 2189

Abstract

Clinical use of 4-Allylpyrocatechol (APC), a potential antifungal agent from Piper betle, is limited because of its low water solubility. The current study explores the development of the self-nanoemulsifying drug delivery system (SNEDDS) containing APC (APC-SNEDDS) to enhance APC solubility. Results demonstrated that excipient type and concentration played an important role in the solubility of APC in the obtained SNEEDS. SNEDDS, comprising 20% Miglyol 812N, 30% Maisine 35-1, 40% Kolliphor RH40, and 10% absolute ethanol, provided the highest loading capacity and significantly increased water solubility of APC. Oil-in-water nanoemulsions (NE) with droplet sizes of less than 40 nm and a narrow size distribution were obtained after dispersing this APC-SNEDDS in water. The droplets had a negative zeta potential between −10 and −20 mV. The release kinetics of APC from APC-SNEDDS followed the Higuchi model. The NE containing 1.6 mg APC/mL had effective activity against Candida albicans with dose-dependent killing kinetics and was nontoxic to normal cells. The antifungal potential was similar to that of 1 mg nystatin/mL. These findings suggest that APC-SNEDDS are a useful system to enhance the apparent water solubility of APC and are a promising system for clinical treatment of oral infection caused by C. albicans. Full article

(This article belongs to the Special Issue Self-Emulsifying Drug Delivery System)

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11 pages, 6811 KiB

Open AccessArticle

Trans-Resveratrol Oral Bioavailability in Humans Using LipiSperse™ Dispersion Technology

by David Briskey and Amanda Rao

Pharmaceutics 2020, 12(12), 1190; https://doi.org/10.3390/pharmaceutics12121190 - 08 Dec 2020

Cited by 16 | Viewed by 3099

Abstract

Resveratrol is a naturally produced compound that has been well researched for its potential health benefits. The primary hindrance towards resveratrol’s therapeutic efficacy is its traditionally poor oral bioavailability. LipiSperse^® is a novel delivery system designed to increase the dispersion of lipophilic ingredients, like resveratrol, in aqueous environments. This single-dose, double-blind, randomized study compared the pharmacokinetics of a commercially available resveratrol with (Veri-Sperse^®) and without (Veri-te) the LipiSperse^® delivery complex. Healthy adults randomly received a single dose of either 150 Veri-te, 75 Veri-Sperse^®, or 150 mg Veri-Sperse^®. Venous blood samples were taken prior to dosing in a fasted state and at 0.5, 1, 2, 3, 4, 5, 6, 8 and 24 h post supplementation. Plasma trans-resveratrol conjugates were measured by liquid-chromatography tandem mass spectrometry (LC-MS/MS). The area under the curve (AUC) (0–24 h), maximum concentration (C_max), and time of maximum concentration (T_max) of plasma conjugates were calculated. The 150 mg dose of Veri-Sperse^® had a 2-fold increase in absorption (AUC) and a 3-fold increase in C_max of trans-resveratrol conjugates compared to 150 mg Veri-te. There was no statistical difference between 75 Veri-Sperse and 150 mg Veri-te for AUC or C_max of resveratrol conjugates. These findings provide support for the use of LipiSperse^® to improve absorption of resveratrol. Full article

(This article belongs to the Special Issue Self-Emulsifying Drug Delivery System)

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23 pages, 2496 KiB

Open AccessArticle

Self-Assembled Cationic-Covered Nanoemulsion as A Novel Biocompatible Immunoadjuvant for Antiserum Production Against Tityus serrulatus Scorpion Venom

by Arthur Sérgio Avelino de Medeiros, Manoela Torres-Rêgo, Ariane Ferreira Lacerda, Hugo Alexandre Oliveira Rocha, Eryvaldo Sócrates Tabosa do Egito, Alianda Maira Cornélio, Denise V. Tambourgi, Matheus de Freitas Fernandes-Pedrosa and Arnóbio Antônio da Silva-Júnior

Pharmaceutics 2020, 12(10), 927; https://doi.org/10.3390/pharmaceutics12100927 - 29 Sep 2020

Cited by 4 | Viewed by 2187

Abstract

This study assesses the efficacy of different nanoemulsion formulations as new and innovative adjuvants for improving the in vivo immunization against the Tityus serrulatus scorpion venom. Nanoemulsions were designed testing key-variables such as surfactants, co-solvents, and the influence of the temperature, which would be able to induce the phase transition from a liquid crystal to a stable nanoemulsion, assessed for four months. Additionally, cationic-covered nanoemulsion with hyper-branched poly(ethyleneimine) was prepared and its performance was compared to the non-cationic ones. The physicochemical properties of the selected nanoemulsions and the interactions among their involved formulation compounds were carefully monitored. The cytotoxicity studies in murine macrophages (RAW 264.7) and red blood cells were used to compare different formulations. Moreover, the performance of the nanoemulsion systems as biocompatible adjuvants was evaluated using mice immunization protocol. The FTIR shifts and the zeta potential changes (from −18.3 ± 1.0 to + 8.4 ± 1.4) corroborated with the expected supramolecular anchoring of venom proteins on the surface of the nanoemulsion droplets. Cell culture assays demonstrated the non-toxicity of the formulations at concentrations less than 1.0 mg/mL, which were able to inhibit the hemolytic effect of the scorpion venom. The cationic-covered nanoemulsion has shown superior adjuvant activity, revealing the highest IgG titer in the immunized animals compared to both the non-cationic counterpart and the traditional aluminum adjuvant. In this approach, we demonstrate the incredible potential application of nanoemulsions as adjuvants, using a nanotechnology platform for antigen delivery system on immune cells. Additionally, the functionalization with hyper-branched poly(ethyleneimine) enhances this recognition and improves its action in immunization. Full article

(This article belongs to the Special Issue Self-Emulsifying Drug Delivery System)

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14 pages, 2878 KiB

Open AccessArticle

In Vitro Evaluation of Self-Nano-Emulsifying Drug Delivery Systems (SNEDDS) Containing Room Temperature Ionic Liquids (RTILs) for the Oral Delivery of Amphotericin B

by Eleni Kontogiannidou, Thomas Meikopoulos, Helen Gika, Emmanuel Panteris, Ioannis S. Vizirianakis, Anette Müllertz and Dimitrios G. Fatouros

Pharmaceutics 2020, 12(8), 699; https://doi.org/10.3390/pharmaceutics12080699 - 25 Jul 2020

Cited by 27 | Viewed by 3610

Abstract

Amphotericin B (AmpB), one of the most commonly used agents in the treatment of severe fungal infections and life-threatening parasitic diseases such as visceral Leishmaniasis, has a negligible oral bioavailability, primarily due to a low solubility and permeability. To develop an oral formulation, medium chain triglycerides and nonionic surfactants in a self-nano-emulsifying drug delivery system (SNEDDS) containing AmpB were combined with room temperature ionic liquids (RTILs) of imidazolium. The presence of ionic liquids significantly enhanced the solubility of AmpB, exhibited a low toxicity and increased the transport of AmpB across Caco-2 cell monolayers. The combination of RTILs with a lipid formulation might be a promising strategy to improve the oral bioavailability of AmpB. Full article

(This article belongs to the Special Issue Self-Emulsifying Drug Delivery System)

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19 pages, 3145 KiB

Open AccessArticle

Development and Evaluation of Docetaxel-Phospholipid Complex Loaded Self-Microemulsifying Drug Delivery System: Optimization and In Vitro/Ex Vivo Studies

by Miao Wang, Sung-Kyun You, Hong-Ki Lee, Min-Gu Han, Hyeon-Min Lee, Thi Mai Anh Pham, Young-Guk Na and Cheong-Weon Cho

Pharmaceutics 2020, 12(6), 544; https://doi.org/10.3390/pharmaceutics12060544 - 12 Jun 2020

Cited by 18 | Viewed by 3105

Abstract

Docetaxel (DTX) has clinical efficacy in the treatment of breast cancer, but it is difficult to develop a product for oral administration, due to low solubility and permeability. This study focused on preparing a self-microemulsifying drug delivery system (SME) loaded with DTX-phospholipid complex (DTX@PLC), to improve the dissolution and gastrointestinal (GI) permeability of DTX. A dual technique combining the phospholipid complexation and SME formulation described as improving upon the disadvantages of DTX has been proposed. We hypothesized that the complexation of DTX with phospholipids can improve the lipophilicity of DTX, thereby increasing the affinity of the drug to the cell lipid membrane, and simultaneously improving permeability through the GI barrier. Meanwhile, DTX@PLC-loaded SME (DTX@PLC-SME) increases the dissolution and surface area of DTX by forming a microemulsion in the intestinal fluid, providing sufficient opportunity for the drug to contact the GI membrane. First, we prepared DTX@PLC-SME by combining dual technologies, which are advantages for oral absorption. Next, we optimized DTX@PLC-SME with nanosized droplets (117.1 nm), low precipitation (8.9%), and high solubility (33.0 mg/g), which formed a homogeneous microemulsion in the aqueous phase. Dissolution and cellular uptake studies demonstrated that DTX@PLC-SME showed 5.6-fold higher dissolution and 2.3-fold higher DTX uptake in Caco-2 cells than raw material. In addition, an ex vivo gut sac study confirmed that DTX@PLC-SME improved GI permeability of DTX by 2.6-fold compared to raw material. These results suggested that DTX@PLC-SME can significantly overcome the disadvantages of anticancer agents, such as low solubility and permeability. Full article

(This article belongs to the Special Issue Self-Emulsifying Drug Delivery System)

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15 pages, 2772 KiB

Open AccessArticle

Development of 20(S)-Protopanaxadiol-Loaded SNEDDS Preconcentrate Using Comprehensive Phase Diagram for the Enhanced Dissolution and Oral Bioavailability

by Young Hoon Kim, Yu Chul Kim, Dong-Jin Jang, Kyoung Ah Min, Jenisha Karmacharya, Thi-Thao-Linh Nguyen, Han-Joo Maeng and Kwan Hyung Cho

Pharmaceutics 2020, 12(4), 362; https://doi.org/10.3390/pharmaceutics12040362 - 15 Apr 2020

Cited by 9 | Viewed by 2651

Abstract

In this study, we aimed to develop a 20(S)-protopanaxadiol (PPD)-loaded self-nanoemulsifying drug delivery system (SNEDDS) preconcentrate (PSP) using comprehensive ternary phase diagrams for enhanced solubility, physical stability, dissolution, and bioavailability. Capmul MCM C8 and Capryol 90 were selected as the oil phase owing to the high solubility of PPD in these vehicles (>15%, w/w). Novel comprehensive ternary phase diagrams composed of selected oil, surfactant, and PPD were constructed, and the solubility of PPD and particle size of vehicle was indicated on them for the effective determination of PSP. PSPs were confirmed via particle size distribution, physical stability, and scanning electron microscope (SEM) with the dispersion of water. The optimized PSP (CAPRYOL90/Kolliphor EL/PPD = 54/36/10, weight%) obtained from the six possible comprehensive ternary phase diagrams showed a uniform nanoemulsion with the particle size of 125.07 ± 12.56 nm without any PPD precipitation. The PSP showed a dissolution rate of 94.69 ± 2.51% in 60 min at pH 1.2, whereas raw PPD showed negligible dissolution. In oral pharmacokinetic studies, the PSP group showed significantly higher C_max and AUC_inf values (by 1.94- and 1.81-fold, respectively) than the raw PPD group (p < 0.05). In conclusion, the PSP formulation with outstanding solubilization, dissolution, and in-vivo oral bioavailability could be suggested using effective and comprehensive ternary phase diagrams. Full article

(This article belongs to the Special Issue Self-Emulsifying Drug Delivery System)

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13 pages, 1553 KiB

Open AccessArticle

RETRACTED: Attenuation of Benign Prostatic Hyperplasia by Optimized Tadalafil Loaded Pumpkin Seed Oil-Based Self Nanoemulsion: In Vitro and In Vivo Evaluation

by Nabil A. Alhakamy, Usama A. Fahmy and Osama A. A. Ahmed

Pharmaceutics 2019, 11(12), 640; https://doi.org/10.3390/pharmaceutics11120640 - 01 Dec 2019

Cited by 21 | Viewed by 4756 | Retraction

Abstract

The FDA has approved tadalafil (TDL) for the treatment of benign prostatic hyperplasia (BPH)-associated symptoms. Pumpkin seed oil (PSO) has shown promise for the relief of prostatitis-related lower urinary tract symptoms. The aim was to improve TDL delivery to the prostate and assess the combined effect of TDL with a PSO-based formula in the management of BPH. PSO, Tween 80, and polyethylene glycol 200 were selected for the optimization of self nano-emulsified drug delivery system (SNEDDS). The formed vesicles were assessed for their globule size and zeta potential. A rat in vivo study was carried out to investigate prostate weight and index, histopathology, and pharmacokinetics. The average globule size for the optimized TDL-PSO SNEDDS was 204.8 ± 18.76 nm, with a zeta-potential value of 7.86 ± 1.21 mV. TDL-PSO SNEDDS produced a marked drop in prostate weight by 35.51% and prostate index by 36.71% compared to the testosterone-only group. Pharmacokinetic data revealed a 2.3-fold increase of TDL concentration, from optimized TDL-PSO SNEDDS, in the prostate compared with the raw TDL group. This study indicated that the combination of TDL and PSO in an optimized TDL PSO SNEDDS formula improved the efficacy of TDL in the management of BPH. Full article

(This article belongs to the Special Issue Self-Emulsifying Drug Delivery System)

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Review

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55 pages, 10800 KiB

Open AccessReview

Self-Nano-Emulsifying Drug-Delivery Systems: From the Development to the Current Applications and Challenges in Oral Drug Delivery

by Aristote B. Buya, Ana Beloqui, Patrick B. Memvanga and Véronique Préat

Pharmaceutics 2020, 12(12), 1194; https://doi.org/10.3390/pharmaceutics12121194 - 09 Dec 2020

Cited by 84 | Viewed by 8721

Abstract

Approximately one third of newly discovered drug molecules show insufficient water solubility and therefore low oral bio-availability. Self-nano-emulsifying drug-delivery systems (SNEDDSs) are one of the emerging strategies developed to tackle the issues associated with their oral delivery. SNEDDSs are composed of an oil phase, surfactant, and cosurfactant or cosolvent. SNEDDSs characteristics, their ability to dissolve a drug, and in vivo considerations are determinant factors in the choice of SNEDDSs excipients. A SNEDDS formulation can be optimized through phase diagram approach or statistical design of experiments. The characterization of SNEDDSs includes multiple orthogonal methods required to fully control SNEDDS manufacture, stability, and biological fate. Encapsulating a drug in SNEDDSs can lead to increased solubilization, stability in the gastro-intestinal tract, and absorption, resulting in enhanced bio-availability. The transformation of liquid SNEDDSs into solid dosage forms has been shown to increase the stability and patient compliance. Supersaturated, mucus-permeating, and targeted SNEDDSs can be developed to increase efficacy and patient compliance. Self-emulsification approach has been successful in oral drug delivery. The present review gives an insight of SNEDDSs for the oral administration of both lipophilic and hydrophilic compounds from the experimental bench to marketed products. Full article

(This article belongs to the Special Issue Self-Emulsifying Drug Delivery System)

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57 pages, 4457 KiB

Open AccessReview

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

by Heejun Park, Eun-Sol Ha and Min-Soo Kim

Pharmaceutics 2020, 12(4), 365; https://doi.org/10.3390/pharmaceutics12040365 - 16 Apr 2020

Cited by 46 | Viewed by 5436

Abstract

Self-emulsifying drug delivery systems (SEDDSs) are a vital strategy to enhance the bioavailability (BA) of formulations of poorly water-soluble compounds. However, these formulations have certain limitations, including in vivo drug precipitation, poor in vitro in vivo correlation due to a lack of predictive in vitro tests, issues in handling of liquid formulation, and physico-chemical instability of drug and/or vehicle components. To overcome these limitations, which restrict the potential usage of such systems, the supersaturable SEDDSs (su-SEDDSs) have gained attention based on the fact that the inclusion of precipitation inhibitors (PIs) within SEDDSs helps maintain drug supersaturation after dispersion and digestion in the gastrointestinal tract. This improves the BA of drugs and reduces the variability of exposure. In addition, the formulation of solid su-SEDDSs has helped to overcome disadvantages of liquid or capsule dosage form. This review article discusses, in detail, the current status of su-SEDDSs that overcome the limitations of conventional SEDDSs. It discusses the definition and range of su-SEDDSs, the principle mechanisms underlying precipitation inhibition and enhanced in vivo absorption, drug application cases, biorelevance in vitro digestion models, and the development of liquid su-SEDDSs to solid dosage forms. This review also describes the effects of various physiological factors and the potential interactions between PIs and lipid, lipase or lipid digested products on the in vivo performance of su-SEDDSs. In particular, several considerations relating to the properties of PIs are discussed from various perspectives. Full article

(This article belongs to the Special Issue Self-Emulsifying Drug Delivery System)

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