Abstract

We here present the synthesis and characterization of a set of biodegradable core–multishell (CMS) nanocarriers. The CMS nanocarrier structure consists of hyperbranched polyglycerol (hPG) as core material, a hydrophobic (12, 15, 18, 19, and 36 C-atoms) inner and a polyethylene glycol monomethyl ether (mPEG) outer shell that were conjugated by ester bonds only to reduce the toxicity of metabolites. The loading capacities (LC) of the drugs, dexamethasone and tacrolimus, and the aggregate formation, phase transitions, and degradation kinetics were determined. The intermediate inner shell length (C15) system had the best overall performance with good LCs for both drugs as well as a promising degradation and release kinetics, which are of interest for dermal delivery.

Highlights

  • Cutaneous drug delivery is the method of choice when skin is the target and systemic side effects are to be avoided

  • The synthesis was reduced to three synthetic steps as compared to synthetic route was established

  • The synthesis was reduced to three synthetic steps as compared six for the amide-based system

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Summary

Introduction

Cutaneous drug delivery is the method of choice when skin is the target and systemic side effects are to be avoided. This is especially the case in inflammatory skin diseases such as psoriasis and atopic dermatitis. The drugs, e.g., the commonly used dexamethasone and tacrolimus, must penetrate the skin first, which is the body’s natural barrier against xenobiotics. The outermost layer, the stratum corneum, has to be overcome to reach the target, namely, the skin’s viable layers. Amphiphiles, among other penetration enhancers, are extensively used to facilitate a deeper penetration [1]. The application of nanoparticles, which have attracted much attention in recent years [2], has been widely explored

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