Abstract
Background: Tacrolimus (TAC) is a drug of natural origin used in conventional topical dosage forms to control atopic dermatitis. However, direct application of the drug often causes adverse side effects in some patients. Hence, drug nanoencapsulation could be used as an improved novel therapy to mitigate the adverse effects and enhance bioavailability of the drug. Methods: Physicochemical properties, in vitro drug release experiments, and in vivo anti-inflammatory activity studies were performed. Results: TAC-loaded nanocapsules were successfully prepared by the interfacial deposition of preformed polymer using poly(ε-caprolactone) (PCL). The nanoparticulate systems presented a spherical shape with a smooth and regular surface, adequate diameter (226 to 250 nm), polydispersity index below 0.3, and suitable electrical stability (−38 to −42 mV). X-ray diffraction confirmed that the encapsulation method provided mainly the drug molecular dispersion in the nanocapsule oily core. Fourier-transform infrared spectra suggested that nanoencapsulation did not result in chemical bonds between drug and polymer. In vitro drug dissolution experiments showed a controlled release with a slight initial burst. The release kinetics showed zero-order kinetics. As per the Korsmeyer–Peppas model, anomalous transport features were observed. TAC-loaded PCL nanocapsules exhibited excellent anti-inflammatory activity when compared to the free drug. Conclusions: TAC-loaded PCL nanocapsules can be suitably used as a novel nano-based dosage form to control atopic dermatitis.
Highlights
Introduction distributed under the terms andAtopic dermatitis (AD), or eczema, is a dermatological, inflammatory, non-infectious, and chronic disease characterized by long-lasting itching of the affected skin and involves a combination of genetic factors that affect the skin barrier and the immune system [1]
The results reported for the inflammatory control group (ICG) represent the typical features of dermatitis, such as the prominent ear swelling and accumulation of inflammatory cells [65]
TAC-loaded polymeric nanocapsules were successfully obtained by the chosen method
Summary
Atopic dermatitis (AD), or eczema, is a dermatological, inflammatory, non-infectious, and chronic disease characterized by long-lasting itching of the affected skin and involves a combination of genetic factors that affect the skin barrier and the immune system [1]. The condition can affect sleep and daily activities leading to discomfort and poor quality of life [1]. The physiopathology of AD is complex, multifactorial, and difficult to understand due to the number of factors that influence it, such as genetic diseases, defects in the epidermal barrier, unsettled immune system, and disturbed skin microbiota [1]. Tacrolimus (TAC) is a drug of natural origin used in conventional topical dosage forms to control atopic dermatitis. Direct application of the drug often causes adverse side effects in some patients. The nanoparticulate systems presented a spherical shape with a smooth and regular surface, adequate diameter (226 to 250 nm), polydispersity index below 0.3, and suitable electrical stability (−38 to −42 mV)
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