Novel microemulsion-based gel formulation of tazarotene for therapy of acne

Abstract

The objective of this study was to develop and evaluate a novel microemulsion based gel formulation containing tazarotene for targeted topical therapy of acne. Psudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant, and co-surfactant for microemulsion formation. The optimized microemulsion formulation containing 0.05% tazarotene was formulated by spontaneous microemulsification method consisting of 10% Labrafac CC, mixed emulsifiers 15% Labrasol-Cremophor-RH 40 (1:1), 15% Capmul MCM, and 60% distilled water (w/w) as an external phase. All plain and tazarotene-loaded microemulsions were clear and showed physicochemical parameters for desired topical delivery and stability. The permeation profiles of tazarotene through rat skin from optimized microemulsion formulation followed the Higuchi model for controlled permeation. Microemulsion-based gel was prepared by incorporating Carbopol®971P NF in optimized microemulsion formulation having suitable skin permeation rate and skin uptake. Microemulsion-based gel showed desired physicochemical parameters and demonstrated advantage over marketed formulation in improving the skin tolerability of tazarotene indicating its potential in improving its topical delivery. The developed microemulsion-based gel may be a potential drug delivery vehicle for targeted topical delivery of tazarotene in the treatment of acne.

Preparation, Characterization and Antioxidant Activity of Xanthone-Loaded Making (Hodgsonia Heteroclita) Microemulsions

“…Moreover, the size of the microemulsion region was affected by the ratio of surfactant to co-surfactant in the order of 2:1>3:1 in agreement with a previous report [20]. The co-surfactants penetrate into the interface between the oil and the water phases, resulting in a decrease in the surface tension, an increase in the flexibility of the surfactant film, and an increase in the water solubility [20,21]. Even oils play an important role in microemulsion due to their effects on the microemulsion area, drug-loading efficiency, and lymphatic transport [22].…”

“…The result shows that the ternary diagram of the Smix of tween 80 and propylene glycol had a wider microemulsion region than that of the Smix of tween 80 and ethanol. Moreover, the size of the microemulsion region was affected by the ratio of surfactant to co-surfactant in the order of 2:1>3:1 in agreement with a previous report [20]. The co-surfactants penetrate into the interface between the oil and the water phases, resulting in a decrease in the surface tension, an increase in the flexibility of the surfactant film, and an increase in the water solubility [20,21].…”

Topically applied lipid- and surfactant-based nanoparticles in the treatment of skin disorders

“…Moreover, these delivery systems are or can be biodegradable and biocompatible, depending on the components used, and are to a significant extent nonimmunogenic and nontoxic. [88] Liposomal gel Liposomal dithranol Psoriasis Market Lifecare Innovations [88] Liposome Nanosomin TM Skin aging Market Elsom Research Innovative Biotechnologies [88] Liposome Equisomin TM Hair root and scalp maintenance Market Elsom Research Innovative Biotechnologies [88] Liposomal gel Ginkgo Skin aging Market Colosé [89] Liposome Whey protein Skin aging Market CLR [90] Liposome Extract of ginkgo, hibiscus and acacia, hyaluronic acid Skin care/aging Market Heliotrop [91,92] Liposome Dermo-Expertise ® Skin care/aging Market L'Oreal [92] Liposome [97] Ethosome Tripeptide-10 citrulline Aged skin Market Genome Cosmetics (ObeyYourBody) [97] Ethosome Noicellex TM Cellulite Market Novel Therapeutic Technologies [47,97] Ethosome Skin Genuity Cellulite Market Physonics [47,97] Ethosome Grape seed Cellulite Market Osmotics cosmeceuticals [47,97] NLC Ubiquinone Aged skin Market Dr. Rimpler [63] NLC Ubiquinone, Titanium dioxide Aged skin Market Dr. Rimpler [63] NLC [44] Niosome Methotrexate Psoriasis Ph II completed - [101] Niosome Urea Psoriasis Ph II completed - [102] Downloaded by [University of Lethbridge] at 08:11 28 June 2016 Niosome Hydroxychloroquine Oral lichen planus Ph II completed - [103] Niosome Ammonium glycyrrhizinate Inflammation Ph I completed - [104,105] Niosome Thai Lanna medicinal plant extracts Alopecia Ph I completed - [106] Niosome High permeation rates In a gel, a higher uptake of the drug in the skin and higher tolerability was shown compared to marketed formulation [86] ME Caprylic/Capric Triglyceride Caprylocaproyl macrogol-8 glyceride PEG-40 hydrogenated castor oil Glyceryl Caprylate/Caprate Tazarotene Acne FDC rat abdominal skin Controlled skin permeation In a gel, suitable skin permeation rate and skin uptake was achieved with increased skin tolerability over commercial product [87] Downloaded by...…”

“…In 2007, a phase III study was completed by MediQuest Therapeutics investigating the transdermal delivery of 1% nitroglycerin in the treatment and prevention of Raynaud's phenomenon [84]. Preclinical research to explore the topical application potential of microemulsions is ongoing, including in the field of nonmelanoma skin cancer and acne [85][86][87] (Table 4).…”

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“…Cumulative amount of drug permeated per unit area versus time graph was plotted, and transdermal flux (J) was calculated from the slope of linear portion [ Figure 2]. [11][12][13][14] …”