Abstract

Dexamethasone-loaded polymer hybrid nanoparticles were developed as a potential tool to treat alopecia areata due to their follicular targeting ability. Freeze drying (FD) is a common technique used to improve nanoparticle stability; however, there are few studies focused on its effect on ethyl cellulose lipid-core nanoparticles. Nanoparticles were lyophilized with different cryoprotectants. Sucrose was selected because it allowed for a good resuspension and provided acceptable physicochemical parameters (374.33 nm, +34.7 mV, polydispersion 0.229%, and 98.87% encapsulation efficiency). The nanoparticles obtained were loaded into a pleasant xanthan gum hydrogel, and the rheological, release, and skin permeation profiles of different formulations were studied. The FD formulation significantly modified the particle size, and the drug release and permeation properties were also altered. In addition, analyses of the cytotoxicity and anti-inflammatory efficacy of FD and non-FD particles on human keratinocytes indicated no differences.

Highlights

  • Nanoparticles have a high surface-to-volume ratio, which is very interesting for topical applications as they increase skin–nanoparticle contact and improve drug diffusion into the skin [1]

  • Freeze drying is a stabilization process in which water is extracted by the sublimation of ice at controlled temperatures and pressures

  • Developed DEX-lipomers composed of ethyl cellulose and medium chain triglycerides were freeze-dried

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Summary

Introduction

Nanoparticles have a high surface-to-volume ratio, which is very interesting for topical applications as they increase skin–nanoparticle contact and improve drug diffusion into the skin [1]. The rigid structure of the nanoparticles facilitates penetration into skin appendages, such as the hair follicles. This follicular targeting acts as a drug reservoir [2], and it is especially interesting to treat diseases related with hair follicles and sebaceous glands, as a result of the accumulation and direct interaction of the drug in the site of action. Alopecia areata is an inflammatory disease that affects between 1% and 2% of the general population [4] It involves hair loss in different patterns (patches of different sizes; alopecia totalis, in which the hair loss affects the entire scalp; and alopecia universalis, involving the loss of body hair), pain, and has a strong emotional impact on the patient.

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