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EMULGELS: A SURROGATE APPROACH FOR TOPICALLY USED HYDROPHOBIC DRUGS
Rachit Khullar*
International Journal of Pharmacy and Biological Sciences , 2011,
Abstract: A unique aspect of dermatological pharmacology is the direct accessibility of the skin as a target organ for diagnosis and treatment. The combination of hydrophilic cornified cells in hydrophobic intercellular material provides a barrier to both hydrophilic and hydrophobic substances. Within the major group of semisolid preparations, the use of transparent gels has expanded both in cosmetics and in pharmaceutical preparations. In spite of many advantages of gels a major limitation is in the delivery of hydrophobic drugs. So to overcome this limitation an emulsion based approach is being used so that even a hydrophobic therapeutic moiety can enjoy the unique properties of gels. When gels and emulsions are used in combined form the dosage forms are referred as emulgels. In recent years, there has been great interest in the use of novel polymers which can function as emulsifiers and thickeners because the gelling capacity of these compounds allows the formulation of stable emulsions and creams by decreasing surface and interfacial tension and at the same time increasing the viscosity of the aqueous phase. In fact, the presence of a gelling agent in the water phase converts a classical emulsion into an emulgel. Emulgels for dermatological use have several favorable properties such as being thixotropic, greaseless, easily spreadable, easily removable, emollient, nonstaining, water-soluble, longer shelf life, bio-friendly, transparent & pleasing appearance. These emulgel are having major advantages on novel vesicular systems as well as on conventional systems in various aspects. Various permeation enhancers can potentiate the effect. So emulgels can be used as better topical drug delivery systems over present systems. The use of emulgels can be extended in analgesics and antifungal drugs.
Nanoparticle Formulation for Hydrophilic & Hydrophobic Drugs
Vivek Kumar Gupta, Alok Gupta,P.K.Karar,S.Ramesh,S.P.Misra
International Journal of Research in Pharmaceutical Sciences , 2010,
Abstract: Nanoparticle formulations have many advantages over traditional dosage forms, such as enhanced dissolution properties and the potential for intracellular drug delivery. Specifically, pure drug nanoparticles, polymeric nanoparticles and polyelectrolyte complexes offer some encouraging results for delivering drugs to various organs and through various routes. Traditional techniques such as spray drying and grinding, and more recent advances in supercritical fluid extraction, precipitation, and double solvent evaporation have been employed to produce nanoparticle formulations for delivery of hydrophilic & hydrophobic drugs here, the benefits of nanoparticle formulations and current progress are compared in light of the practical encumbrances of producing formulations, and possible toxicological effects of these materials.
EMULGEL: A COMPREHENSIVE REVIEW ON THE RECENT ADVANCES IN TOPICAL DRUG DELIVERY  [PDF]
Joshi Baibhav,Singh Gurpreet,Rana A.C,Saini Seema
International Research Journal of Pharmacy , 2011,
Abstract: Emulgel has emerged as a promising drug delivery system for the delivery of hydrophobic drugs. When gel and emulsion are used in combined form they are referred as Emulgel. Emulsion in gel have emerged as one of the most interesting topical drug delivery system as it have dual release control system i.e. emulsion and gel. Gels are relatively newer class of dosage form created by entrapment of large amount of aqueous or hydro alcoholic liquid in a network of colloidal solid particles which may consist of inorganic substances or organic polymers of natural or synthetic origin. In recent years there has been great interest in the use of novel polymers with complex function such as emulsifiers and thickeners. The gelling capacity of these compounds allows the formulation of stable emulsion and creams by decreasing surface and interfacial tension at the same time increasing the viscosity of aqueous phase. In spite of many advantages of gels a major limitation is in the delivery of hydrophobic drug. So to overcome this limitation an emulsion based approach is being used so that even a hydrophobic moiety can enjoy the unique property of gel.
New Formulation Strategies in Topical Antifungal Therapy  [PDF]
Sevgi Güng?r, M. Sedef Erdal, Buket Aksu
Journal of Cosmetics, Dermatological Sciences and Applications (JCDSA) , 2013, DOI: 10.4236/jcdsa.2013.31A009
Abstract:

Fungal infections of the skin are one of the often faced with dermatological diseases in worldwide. Topical therapy is an attractive choice for the treatment of the cutaneous infections due to its advantageous such as targeting of drugs to the site of infection and reduction of the risk of systemic side effects. Currently, antifungal drugs are generally used as conventional cream and gel preparations in topical treatment. The efficiency of that treatment depends on the penetration of drugs through the target layers of the skin at the effective concentrations. However, stratum corneum, the outermost layer of the skin, is an effective barrier for penetration of drugs into deeper layers of the skin. The physicochemical characteristics of drug molecules and the types of the formulations are effective factors in topical drug delivery. Therefore, a number of formulation strategies have been investigated for delivering antifungal compounds through targeted site of the skin. This review article focuses on the new alternative formulation approaches to improve skin penetration of antifungal drugs.

FORMULATION AND DEVELOPMENT OF LIPOSOMAL GEL FOR TOPICAL DRUG DELIVERY SYSTEM
Suraj R. Wasankar*, Syed M. Faizi and Abhisek D. Deshmuk
International Journal of Pharmaceutical Sciences and Research , 2012,
Abstract: Aim: The aims of this study were to develop liposome enriched Dexibuprofen liposomal hydrogels for topical delivery, perform in vitro release studies and in vivo permeation studies through mice/rat skin, and evaluate the efficacy of liposomal gels against inflammation induced rats. The purpose was to provide the delivery of the topical drug at a sustained rate across intact skin to improve bioavailability and inflammation control for longer period from liposomal gels.Method: Phosphatidylcholine, Cholesterol and Dexibuprofen were dissolved in chloroform/methanol (2:1, v/v) mixture and subsequently transferred into a pear-shaped flask connected to a Rotavapor (Büchi- type). Rotary evaporation method was used for the formulation of liposomes.Result: liposome prepared was evaluated for particle size measurement, percent drug entrapment, diffusion study, skin permeation study and in vivo study. F-7 batch found to be optimized batch having particle size 5.40 μm, % drug entrapment 61.70, % CDR 75.35 %. Hence F-7 batch further evaluated for skin permeation study, skin deposition study, in vivo study and stability study.Conclusion: The present study has been a satisfactory attempt to formulate and evaluate liposome of Dexibuprofen and liposomal gel with a providing sustained delivery of drug. From skin permeation study and in vivo study it was concluded that the prepared liposome of Dexibuprofen may prove to be potential candidate for safe and effective sustained drug delivery over an extended period of time which can reduce dosing frequency.
Review: REVIEW ON SOLUBILITY ENHANCEMENT TECHNIQUES FOR HYDROPHOBIC DRUGS  [PDF]
Anuj Kumar*,Sangram Keshri Sahoo,Kumud Padhee,Prithi Pal Singh Kochar
Pharmacie Globale : International Journal of Comprehensive Pharmacy , 2011,
Abstract: Among all newly discovered chemical entities about 40% drugs are lipophillic and fail to reach market due to their poor aqueous solubility. For orally administered drugs solubility is one of the rate limiting parameter to achieve their desired concentration in systemic circulation for pharmacological response. Problem of solubility is a major challenge for formulation scientist, which can be solved by different technological approaches during the pharmaceutical product development. Solid dispersion, Micronization, Salt formation, are some of the vital approaches routinely employed to enhance the solubility of poorly soluble drugs but each approach has some limitation and advantages. Novel techniques like Nano-suspension, Supercritical processing, Cryogenic technology may allow greater opportunities in the delivery of poorly soluble drugs. The solubility behavior of drugs remains one of the most challenging aspects in formulation development. The present review is devoted to various traditional and novel techniques for enhancing drug solubility to reduce the percentage of poorly soluble drug candidates eliminated from the development.
Topical Drug Delivery Systems : A Review  [cached]
Mr.J.P.Goswami,Shailesh Sharma,Dr.G.D.Gupta,Mr.Anis Mustafa
Pharmaceutical Reviews , 2008,
Abstract: Topical preparations are used for the localized effects at the site of their application by virtue of drug penetration into the underlying layers of skin or mucous membranes.The main advantage of topical delivery system is to bypass first pass metabolism. Avoidance of the risks and inconveniences of intravenous therapy and of the varied conditions of absorption, like pH changes, presence of enzymes, gastric emptying time are other advantage of topical preparations. Semi-solid formulation in all their diversity dominate the system for topical delivery, but foams, spray, medicated powders, solution, and even medicated adhesive systems are in use. The topical drug delivery system is generally used where the others system of drug administration fails or it is mainly used in pain management, contraception, and urinary incontinence. This review describes the various formulation aspects, various excipients, evaluation tests, challenges and drugs explored in the field of topical drug delivery.
Formulation and Evaluation of Topical Hydrogel Patch Containing Amide Type Local Anaesthetic Agent
Jayrajsinh Sarvaiya,Chintan Tank,Kosanam Divakar,Jay Upadhyay
International Journal For Pharmaceutical Research Scholars , 2012,
Abstract: Hydrogel based drug delivery systems provides significant effect in designing sustained release topical dosage forms. Topical patch containing drug in hydrogel type polymer matrix provides not only targeted drug flux through the skin but also provides cooling effect on application site. Topical hydrogel patch containing lidocaine was prepared by using sodium poly acrylate as bioadhesive polymer. Effect of brij 30 and transcutol was also evaluated on topical flux of lidocaine base from hydrogel patch. Transcutol (10% w/w) provides sufficient drug release in contrast to brij 30(4%w/w) in prepared hydrogel patches. Maintenance of uniformity of weight is one of the critical task in preparation of hydrogel patch as polymers used are highly water absorbent. Excess amount of penetration enhancers leads to alter adhesive property of bioadhesive patch so formulation was optimized with Sodium polyacrylate (7%w/w) as the desired concentration for necessary bioadhesiveness and zinc oxide as cross linking agent.
Self-assembled rosette nanotubes for incorporating hydrophobic drugs in physiological environments  [cached]
Shang Song,Yupeng Chen,Zhimin Yan,et al
International Journal of Nanomedicine , 2011,
Abstract: Shang Song1, Yupeng Chen1,2, Zhimin Yan4, Hicham Fenniri4, Thomas J Webster1,31School of Engineering, 2Department of Chemistry, 3Department of Orthopaedics, Brown University, Providence, RI, USA; 4National Institute for Nanotechnology and Department of Chemistry, National Research Council and University of Alberta, Edmonton, CanadaAbstract: Rosette nanotubes (RNTs) are novel, biomimetic, injectable, self-assembled nanomaterials. In previous studies, materials coated with RNTs have significantly increased cell growth (eg, osteoblasts, chondrocytes, and endothelial cells) due to the favorable cellular environment created by RNTs. It has also been suggested that the tubular RNT structures formed by base stacking and hydrophobic interactions can be used for drug delivery, and this possibility has not been studied to date. Here we investigated methods to load and deliver tamoxifen (TAM, a hydrophobic anticancer drug) using two different types of RNTs: single-base RNTs and twin-base RNTs. Drug-loaded RNTs were characterized by nuclear magnetic resonance spectroscopy, diffusion-ordered nuclear magnetic resonance spectroscopy (DOSY NMR), and ultraviolet-visible (UV-Vis) spectroscopy at different ratios of twin-base RNTs to TAM. The results demonstrated successful incorporation of hydrophobic TAM into RNTs. Importantly, because of the hydrophilicity of the outer surface of the RNTs, TAM-loaded RNTs were dissolved in water, and thus have great potential to deliver hydrophobic drugs in various physiological environments. The results also showed that twin-base RNTs further improved TAM loading. Therefore, this study demonstrated that hydrophobic pharmaceutical agents (such as TAM), once considered hard to deliver, can be easily incorporated into RNTs for anticancer treatment purposes.Keywords: drug delivery, rosette nanotubes, self-assembly, tamoxifen
Self-assembled rosette nanotubes for incorporating hydrophobic drugs in physiological environments
Shang Song, Yupeng Chen, Zhimin Yan, et al
International Journal of Nanomedicine , 2011, DOI: http://dx.doi.org/10.2147/IJN.S11957
Abstract: ssembled rosette nanotubes for incorporating hydrophobic drugs in physiological environments Original Research (5121) Total Article Views Authors: Shang Song, Yupeng Chen, Zhimin Yan, et al Published Date January 2011 Volume 2011:6 Pages 101 - 107 DOI: http://dx.doi.org/10.2147/IJN.S11957 Shang Song1, Yupeng Chen1,2, Zhimin Yan4, Hicham Fenniri4, Thomas J Webster1,3 1School of Engineering, 2Department of Chemistry, 3Department of Orthopaedics, Brown University, Providence, RI, USA; 4National Institute for Nanotechnology and Department of Chemistry, National Research Council and University of Alberta, Edmonton, Canada Abstract: Rosette nanotubes (RNTs) are novel, biomimetic, injectable, self-assembled nanomaterials. In previous studies, materials coated with RNTs have significantly increased cell growth (eg, osteoblasts, chondrocytes, and endothelial cells) due to the favorable cellular environment created by RNTs. It has also been suggested that the tubular RNT structures formed by base stacking and hydrophobic interactions can be used for drug delivery, and this possibility has not been studied to date. Here we investigated methods to load and deliver tamoxifen (TAM, a hydrophobic anticancer drug) using two different types of RNTs: single-base RNTs and twin-base RNTs. Drug-loaded RNTs were characterized by nuclear magnetic resonance spectroscopy, diffusion-ordered nuclear magnetic resonance spectroscopy (DOSY NMR), and ultraviolet-visible (UV-Vis) spectroscopy at different ratios of twin-base RNTs to TAM. The results demonstrated successful incorporation of hydrophobic TAM into RNTs. Importantly, because of the hydrophilicity of the outer surface of the RNTs, TAM-loaded RNTs were dissolved in water, and thus have great potential to deliver hydrophobic drugs in various physiological environments. The results also showed that twin-base RNTs further improved TAM loading. Therefore, this study demonstrated that hydrophobic pharmaceutical agents (such as TAM), once considered hard to deliver, can be easily incorporated into RNTs for anticancer treatment purposes.
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