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®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 microemulsion-based gel may be a potential drug delivery vehicle for targeted topical delivery of isotretinoin in the treatment of acne.
Highlights
Acne, a cutaneous disorder of multifactorial origin, is a disease whose cause and severity depend on the relationship between hormones, keratinization, sebum and bacteria
An ongoing trial in patients with antibiotic-resistant P. acnes indicates that ITTN is highly effective; treatment of P. acnes may well become a new indication for this drug (Zaenglein 2008)
It has been reported that the large solubilizing capacity of ME leads to larger concentration gradient toward the skin, providing superior dermal flux, for which high solubility of ITTN in oily phase can be an added advantage to increase it in ME
Summary
A cutaneous disorder of multifactorial origin, is a disease whose cause and severity depend on the relationship between hormones, keratinization, sebum and bacteria. Isotretinoin (ITTN), a derivative of retinoic acid (13-cisretinoic acid), is the most effective compound with potential to suppress acne over the long term (Zaenglein 2008; Patel et al 2011a). It appears to derive its effectiveness from increased production of the antimicrobial protein neutrophil gelatinase-associated lipocalin in the skin reducing sebum levels and in turn reducing levels of Propionibacterium acnes (P. acnes). ITTN, reducing the growth of P.acnes in a secondary manner, was selected for further study Despite these interesting features, extremely low solubility limits ITTN incorporation into an acceptable vehicle and its tolerability results in either discontinuation of treatment or
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