Biocompatible Microemulsions and Their Prospective Uses in Drug Delivery

Gupta, Syamasri; Moulik, Satya P.

doi:10.1002/jps.21177

Cited by 167 publications

(91 citation statements)

References 117 publications

(143 reference statements)

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“…Based on the high drug solubility, which was important to achieve, benzyl alcohol, oleic acid, and lemon oil were selected for preparation of the CTM microemulsions (24). Although the drug had a relative low solubility in IPM compared to other oils, it was also selected for the preparation of microemulsions due to its well-known permeation-enhancing property (25) and biocompatibility (26).…”

Section: Determination Of Saturation Solubility Of Ctm In Different Oilsmentioning

confidence: 99%

Formulation, Characterization, and Clinical Evaluation of Microemulsion Containing Clotrimazole for Topical Delivery

et al. 2011

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Abstract. The objective of the present study was to formulate and evaluate microemulsion systems for topical delivery of clotrimazole (CTM). The solubility of CTM in various oils was determined to select the oil phase of the microemulsion systems. Pseudoternary phase diagrams were constructed to identify the area of microemulsion existence. Five CTM microemulsion formulations (M1-M5) were prepared and evaluated for their thermodynamic stability, pH, refractive index, droplet size, viscosity, and in vitro release across cellulose membrane. Among the prepared microemulsion formulations, M3 (lemon oil/ Tween 80/n-butanol/water) and M4 (isopropyl myristate/Tween 80/n-butanol/water) microemulsion systems were found to be promising according to their physical properties and CTM cumulative percentage release. Gel form of M3 and M4 were prepared using 1% Carbopol 940 as the hydrogel matrix. Both formulations were evaluated in the liquid and gel forms for drug retention in the skin in comparison to the marketed CTM topical cream and their stability examined after storage at 40°C for 6 months. Microemulsion formulations achieved significantly higher skin retention for CTM over the CTM cream. Stability studies showed that M4 preparations were more stable than M3. The in vitro antifungal activity of M4 against Candida albicans was higher than that of the conventional cream. Moreover, clinical evaluation proved the efficacy and tolerability of this preparation in the treatment of various topical fungal infections.

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Section: Determination Of Saturation Solubility Of Ctm In Different Oilsmentioning

confidence: 99%

Formulation, Characterization, and Clinical Evaluation of Microemulsion Containing Clotrimazole for Topical Delivery

et al. 2011

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“…23) In addition, combinations of a high HLB surfactant and lower HLB surfactants have often been used for preparation of emulsions of lipophilic compounds. 24,25) Based on results of those studies, an emulsion composed of appropriate components and an appropriate combination of surfactants would improve intestinal absorption of such highly lipophilic compounds. Taking into account the safety of these components, further investigations to establish evidence of pharmaceutical design for theoretical improvement of intestinal absorption of these compounds are in progress.…”

Section: Fig 3 Plasma Concentrations Of Coq10 In Rats After Oral Admentioning

confidence: 99%

Emulsification Using Highly Hydrophilic Surfactants Improves the Absorption of Orally Administered Coenzyme Q10

Sato

Mutoh

Suzuki

et al. 2013

Biological & Pharmaceutical Bulletin

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Coenzyme Q10 (CoQ10) is an essential component in the electron-transport systems of mitochondria and bacteria and is often used as a supplementary treatment for some diseases. We previously reported that the bioavailability of CoQ10 powder was less than 10%. In this study, we investigated various preparations to improve the intestinal absorption of CoQ10 with focus on the effect of emulsification. We prepared a suspension and some emulsions with four types of surfactants and investigated the plasma concentration profile after oral administration to rats. The absorption of CoQ10 was improved by an emulsion formulation although there was little absorption of CoQ10 when a suspension was administered. However, little CoQ10 was absorbed in the bile duct-ligated group even when the emulsion formulation was administered (about 50% of the control group). Bile and emulsion formulation are essential for absorption of CoQ10. When the preparations containing Tween20 (polysorbate (20) sorbitan monolaurate) and Tween80 (polyoxyethylene (20) sorbitan monooleate) were administered, plasma concentrations of CoQ10 were higher than those obtained with preparations containing Tween65 (polyoxyethylene (20) sorbitan tristearate) and Span20 (sorbitan monolaurate). Tween20 and Tween80 have higher hydrophile-lipophile balance (HLB) values than those Tween65 and Span20. Our study suggests that highly lipophilic compounds like CoQ10 would diffuse the unstirred water layer and would easily access the intestinal apical membrane by an emulsion containing a surfactant with a high HLB value. Attention must be given to CoQ10 supplementation for patients whose bile is not excreted to the intestine such as patients with cholestasis.Key words coenzyme Q10; absorption; bile; emulsion; intestine; lutein Preventive medicine and anti-aging medicine have received much attention recently due to increases in the proportion of elderly people in the population and patients with lifestyle diseases such as hypertension, dislipidemia and diabetes. Oxidative stress is involved in the onset of lifestyle diseases, 1,2) and various antioxidant supplements and antioxidant-fortified functional foods have recently become available. Many epidemiological studies have shown relationships between consumption of polyphenol or carotenoid-rich foods and prevention of these lifestyle diseases. 3,4) Coenzyme Q (CoQ) has a benzoquinone ring linked to a polyisoprenyl chain of 9 or 10 units in mammalian species. CoQ10, also known as ubiquinone, is a ubiquitous component vital to a number of activities related to energy metabolism. CoQ10 also functions in its reduced form as an antioxidant, protecting biological membranes and serum low density lipoprotein (LDL) from lipid peroxidation. 5,6) The use of CoQ10 as a therapeutic cardiovascular agent was based on its fundamental role in mitochondrial function and cellular bioenergetics. 7,8) Many studies have also indicated a beneficial antioxidant effect of CoQ10 as supplementation, and CoQ10 has received much attention due to its an...

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“…Several hypotheses have been put forward for the mechanism of drug permeation enhancement. These include increased drug solubility, which fosters a high concentration gradient towards skin, small droplet size and low viscosity which facilitates permeation, increased drug thermodynamic activity in the microemulsion vehicle, and the disruption of the stratum corneum lipid order by microemulsion components (Kreilgaard, 2002;Zhao et al, 2006;Biruss, Kählig, Valenta, 2007;Gupta, Moulik, 2008;Vicentini et al, 2008;Moniruzzaman, Kamiya, Goto, 2010;Shakeel, Ramadan, 2010).…”

Section: Introductionmentioning

confidence: 99%

Microemulsion based on Pterodon emarginatus oil and its anti-inflammatory potential

Pascoa

Diniz

Florentino

et al. 2015

Braz. J. Pharm. Sci.

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This article reports the development of a pharmaceutical product containing vegetable actives from a Brazilian medicinal plant. The possibility of forming a microemulsion using Pterodon emarginatus ("sucupira") oil was evaluated and the anti-inflammatory potential of this microemulsion was also examined. A formulation was developed using P. emarginatus oil, a mixture of ethoxylated Castor Oil (Ultramone ® R-540/propylene glycol 2:1) (surfactant/cosurfactant) and distilled water at a ratio of 10:15:75, respectively. The microemulsion which was selected was then subjected to the preliminary stability test and analyzed in terms of average diameter of droplets, pH, zeta potential, and polydispersity index, on the 1 st , 7 th , 15 th , and 30 th days after preparation and stored at different temperatures (5 ± 2 °C, 25 ± 2 °C, and 40 ± 2 °C). The anti-inflammatory in vivo activity of both oil and formulation were evaluated, using the experimental model of croton oil-induced ear edema. The preliminary stability test showed that the microemulsion stored at 5 and 25 °C retained its original features throughout the 30-day period. The anti-inflammatory potential of both oil and formulation was shown to be statistically significant (p < 0.001), when compared to the control group, however, the microemulsion proved to be more effective (p < 0.05) than the oil when applied directly to the ear. Descrevemos o desenvolvimento de um produto farmacêutico contendo ativo vegetal baseado em uma planta medicinal brasileira. Foi avaliada a habilidade de formação de uma microemulsão à base do óleo de Pterodon emarginatus (sucupira) e seu potential anti-inflamatório. Uma formulação foi desenvolvida utilizando o óleo de P. emarginatus, mistura de óleo de mamona etoxilado (Ultramona ® R-540)/propilenoglicol (2:1) (tensoativo/cotensoativo) e água destilada, na proporção de 10:15:75, respectivamente. A microemulsão selecionada foi submetida ao teste preliminar de estabilidade e foi analisada quanto ao diâmetro médio das gotículas, pH, potential zeta e índice de polidispersão, no 1º, 7º, 15º e 30º dias após o preparo e foram estocadas em diferentes temperaturas (5±2 °C, 25±2 °C e 40±2 °C). Avaliaram-se a atividade anti-inflamatória in vivo do óleo de sucupira e da formulação, usando o modelo experimental do edema de orelha induzido pelo óleo de cróton. No teste preliminar de estabilidade observou-se que a formulação estocada a 5 °C e a 25 °C mantiveram suas características originais durante 30 dias. O potencial anti-inflamatório de ambos, óleo de sucupira e formulação foi estatisticamente significativo (p <0.001), quando comparado ao controle, porém a microemulsão foi mais eficiente (p <0.05) que o óleo aplicado diretamente nas orelhas dos animais. Unitermos:Pterodon emarginatus/pharmacognosy. Pterodon emarginatus/óleo/atividade antiinflamatória. Plantas medicinais. Microemulsão. Fitoterápico. Tecnologia farmacêutica.

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Biocompatible Microemulsions and Their Prospective Uses in Drug Delivery

Cited by 167 publications

References 117 publications

Formulation, Characterization, and Clinical Evaluation of Microemulsion Containing Clotrimazole for Topical Delivery

Formulation, Characterization, and Clinical Evaluation of Microemulsion Containing Clotrimazole for Topical Delivery

Emulsification Using Highly Hydrophilic Surfactants Improves the Absorption of Orally Administered Coenzyme Q10

Microemulsion based on Pterodon emarginatus oil and its anti-inflammatory potential

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