Formulation development of ethosomes containing indomethacin for transdermal delivery

Sakdiset, Pajaree; Amnuaikit, Thanaporn; Pichayakorn, Wiwat; Pinsuwan, Sirirat

doi:10.1016/j.jddst.2019.05.048

Cited by 45 publications

(23 citation statements)

References 43 publications

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“…On the other hand, it was noticed that upon increasing X 2 from 3.96 to 11%, a subsequent decrease in the ethosomal vesicular size from 218 to 118 nm for F12 and F10, respectively, was recorded. A reverse action was observed for ethanol concentration variable X 2 which points toward decreasing the vesicular size because of the great stabilization provided to the ethosome that resulted in smaller vesicular size [ 28 ]. The influence of both independent variables X 1 and X 2 on the BRU loaded ethosome vesicular size (Y 1 ) is visibly explained through 2D contour and 3D-response surface plot as displayed in Figure 1 A,B.…”

Section: Resultsmentioning

confidence: 99%

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Quality by Design for Development, Optimization and Characterization of Brucine Ethosomal Gel for Skin Cancer Delivery

et al. 2021

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Natural products have been extensively used for treating a wide variety of disorders. In recent times, Brucine (BRU) as one of the natural medications extracted from seeds of nux vomica, was investigated for its anticancer activity. As far as we know, this is the first study on BRU anticancer activity against skin cancer. Thus, the rational of this work was implemented to develop, optimize and characterize the anticancer activity of BRU loaded ethosomal gel. Basically, thin film hydration method was used to formulate BRU ethosomal preparations, by means of Central composite design (CCD), which were operated to construct (32) factorial design. Two independent variables were designated (phospholipid percentage and ethanol percentage) with three responses (vesicular size, encapsulation efficiency and flux). Based on the desirability function, one formula was selected and incorporated into HPMC gel base to develop BRU loaded ethosomal gel. The fabricated gel was assessed for all physical characterization. In-vitro release investigation, ex-vivo permeation and MTT calorimetric assay were performed. BRU loaded ethosomal gel exhibited acceptable values for the characterization parameters which stand proper for topical application. In-vitro release investigation was efficiently prolonged for 6 h. The flux from BRU loaded ethosome was enhanced screening optimum SSTF value. Finally, in-vitro cytotoxicity study proved that BRU loaded ethosomal gel significantly improved the anticancer activity of the drug against A375 human melanoma cell lines. Substantially, the investigation proposed a strong motivation for further study of the lately developed BRU loaded ethosomal gel as a prospective therapeutic strategy for melanoma treatment.

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Section: Resultsmentioning

confidence: 99%

“…BRU loaded ethosome was prepared by thin film hydration method that reported previously by Sakdiset et al [ 28 ]. Concisely, BRU (50 mg) was used in addition to same amount of cholesterol and both were added into clean, desiccated round bottomed flask.…”

Section: Methodsmentioning

confidence: 99%

Quality by Design for Development, Optimization and Characterization of Brucine Ethosomal Gel for Skin Cancer Delivery

et al. 2021

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“…Ethosomes were deemed to possess better biocompatibility and higher drug permeabilities, compared to conventional liposomes [105]. Some representative drugs which have been successfully delivered using ethosomes include the following: apigenin [106], valsartan [107], econazole nitrate [108], quercetin [109], indometacin [110], curcumin [111], green tea extract [112] and mitoxantrone [113]. A modification of ethosomes, namely transethosome, was introduced by Song et al [114] who combined the use of phospholipids, with high amounts of ethanol and surfactant, acting as permeation enhancers, for delivery of voriconazole.…”

Section: Vesicles and Analoguesmentioning

confidence: 99%

Enhancement strategies for transdermal drug delivery systems: current trends and applications

Ramadon

McCrudden

Courtenay

et al. 2021

Drug Deliv. and Transl. Res.

246

159

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Transdermal drug delivery systems have become an intriguing research topic in pharmaceutical technology area and one of the most frequently developed pharmaceutical products in global market. The use of these systems can overcome associated drawbacks of other delivery routes, such as oral and parenteral. The authors will review current trends, and future applications of transdermal technologies, with specific focus on providing a comprehensive understanding of transdermal drug delivery systems and enhancement strategies. This article will initially discuss each transdermal enhancement method used in the development of first-generation transdermal products. These methods include drug/vehicle interactions, vesicles and particles, stratum corneum modification, energy-driven methods and stratum corneum bypassing techniques. Through suitable design and implementation of active stratum corneum bypassing methods, notably microneedle technology, transdermal delivery systems have been shown to deliver both low and high molecular weight drugs. Microneedle technology platforms have proven themselves to be more versatile than other transdermal systems with opportunities for intradermal delivery of drugs/biotherapeutics and therapeutic drug monitoring. These have shown that microneedles have been a prospective strategy for improving transdermal delivery systems. Graphical abstract

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“…In order to overcome the mentioned limitations, the development of novel indomethacin topical formulations with higher skin penetration efficiency is required. Sakdiset et al [ 61 ] as the solution for this problem proposed the ethosomes containing indomethacin. They developed the method of obtaining the ethosomes with good colloidal appearance using various concentrations of soybean phosphatidylcholine, ethanol, and dispersing agents and test them in an in vitro model on pig skin.…”

Section: Novel Strategies For Indomethacin Deliverymentioning

confidence: 99%

“…Prepared ethosomes led to significantly higher permeation of IND through pig skin over 24 h than the commercial solution and the ethanolic solution of indomethacin. Moreover, ethosomes were stable in terms of physical appearance, drug content, and entrapment efficiency (EE) during storage at ambient temperature for 3 months, ensuring greater permeability of indomethacin through the skin than a commercial solution of this drug or a prepared ethanolic solution, which indicates that it is possible to use this form of formulation as transdermal carriers for this drug [ 61 ].…”

Section: Novel Strategies For Indomethacin Deliverymentioning

confidence: 99%

Lipid Formulations and Bioconjugation Strategies for Indomethacin Therapeutic Advances

Gliszczyńska

Nowaczyk

2021

Molecules

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Indomethacin (IND) is a drug which after successful clinical trials became available for general prescription in 1965 and from that time is one of the most widely used anti-inflammatory drug with the highest potencies in the in vitro and in vivo models. However, despite its high therapeutic efficacy in relieving the symptoms of certain arthritis and in treating gout or collagen diseases, administration of IND causes a number of adverse effects, such as gastrointestinal ulceration, frequent central nervous system disorders and renal toxicity. These obstacles significantly limit the practical applications of IND and make that 10–20% of patients discontinue its use. Therefore, during the last three decades many attempts have been made to design novel formulations of IND aimed to increase its therapeutic benefits minimizing its adverse effects. In this review we summarize pharmacological information about IND and analyze its new lipid formulations and lipid bioconjugates as well as discuss their efficacy and potential application.

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Formulation development of ethosomes containing indomethacin for transdermal delivery

Cited by 45 publications

References 43 publications

Quality by Design for Development, Optimization and Characterization of Brucine Ethosomal Gel for Skin Cancer Delivery

Quality by Design for Development, Optimization and Characterization of Brucine Ethosomal Gel for Skin Cancer Delivery

Enhancement strategies for transdermal drug delivery systems: current trends and applications

Lipid Formulations and Bioconjugation Strategies for Indomethacin Therapeutic Advances

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