Abstract
Few topical products have been developed specifically to treat acute and chronic arthritis and inflammation, using non-steroidal anti-inflammatory drugs (NSAIDs). The lack of dosing accuracy commonly found in locally applied semisolid products for cutaneous use is a critical issue that leads to treatment failure. The aim of the present work is to develop a differentiated and innovative topical patch based on a monolithic hydrogel for ibuprofen skin delivery, in order to provide a safer and accurate way of drug administration along with improved treatment compliance. Topical patches based on hydroxypropylmethylcellulose (HPMC) were optimized in composition, in terms of enhancer and adhesive, supported on a systematic assessment of in vitro release and permeation behavior and adhesion properties. Several mathematical models were used to scrutinize the release mechanisms from the patches. In vitro release kinetics was shown to be mainly driven by diffusion. However, other mechanisms seemed to be also present, supporting the feasibility of using patches for sustained drug delivery. PEG 200 provided the best permeation rate, with a permeation enhancement ratio of ca. 3 times higher, than the commercial reference. The addition of Eudragit L30D 55 to the formulation led to the best adhesion profile, thus achieving a successful development based on a safe-by-design concept.
Highlights
The skin is the largest organ of the human body and a key barrier in drug delivery
A systematic development approach based on the assessment of release, permeation behavior and adhesion properties, as critical quality attributes (CQAs), was taken into consideration to consistently deliver the intended performance of the product
The patch preparation began with a solution of HPMC (1.5% w/w) prepared under mechanical stirring at 80 oC, lower temperatures were previously considered, since this parameter is closely related to the polymer concentration
Summary
The skin is the largest organ of the human body and a key barrier in drug delivery It is structured into three main layers: the epidermis, dermis and hypodermis. (Benson and Watkinson, 2012) This layer represents a challenging physical barrier, regulating water loss from the body, preventing permeation of microorganisms of the skin surface and restricting passive drug diffusion. Topical products exhibit advantages regarding the oral formulations, since they can overcome first-pass metabolism and the adverse gastrointestinal tract environment, which is associated to pH variation, enzymatic activity and drug interaction with food and drinks (Prausnitz and Langer, 2008).
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