Novel isotretinoin microemulsion-based gel for targeted topical therapy of acne: formulation consideration, skin retention and skin irritation studies

Abstract

Isotretinoin was formulated in novel microemulsion-based gel formulation with the aim of improving its solubility, skin tolerability, therapeutic efficacy, skin-targeting efficiency and patient compliance. Microemulsion was formulated by the spontaneous microemulsification method using 8 % isopropyl myristate, 24 % Labrasol, 8 % plurol oleique and 60 % water as an external phase. All plain and isotretinoin-loaded microemulsions were clear and showed physicochemical parameters for the desired topical delivery and stability. The permeation profiles of isotretinoin through rat skin from selected microemulsion formulation followed zero-order kinetics. Microemulsion-based gel was prepared by incorporating Carbopol Ò 971 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 isotretinoin, indicating its potential in improving topical delivery of isotretinoin. The developed microemulsionbased gel may be a potential drug delivery vehicle for targeted topical delivery of isotretinoin in the treatment of acne.

A novel hydrogel-thickened microemulsion of dapsone for acne treatment: Development, characterization, physicochemical stability and ex vivo permeation studies

“…IPM is one of the most common ingredients in skin care products with emollient properties [22] that could be helpful to reduce skin dryness, the most common side effect of dapsone marketed topical application [23]. Moreover, it has been used previously in the anti-acne topical formulations [24]. Menthol is a safe cyclic monoterpene alcohol with a pleasant odor which possesses anti-inflammatory characteristics [25].…”

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

“…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).…”

“…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...…”

Preparation and in vitro/ex vivo evaluation of nanoemulsion for transnasal delivery of paliperidone

“…The infrared (IR) spectra (between 4000 and 400 cm -1 ) of PALI, plain NE, optimized PNE6 and PMNE6 were taken using an IR spectrophotometer (Spectrum GX FT-IR, Perkin Elmer, Norwalk, CT) to detect any possible interaction between the drug and excipients (Patel et al 2009(Patel et al , 2015.…”

“…Further, it is reported in the literature that oleic acid act as a lipophilic permeation enhancer and can be useful to improve the membrane permeability (Azeem et al 2009;Patel et al 2015;Pierre et al 2006). Hence, oleic acid was selected as the oily phase for the preparation of NE (Pierre et al 2006).…”