Topical Artocarpus communis Nanoparticles Improved the Water Solubility and Skin Permeation of Raw A. communis Extract, Improving Its Photoprotective Effect.

Chun-Yin Yang,Pao-Hsien Huang,Feng-Lin Yen,Chih-Hua Tseng

doi:10.3390/pharmaceutics13091372

Abstract

Antioxidants from plant extracts are often used as additives in skincare products to prevent skin problems induced by environmental pollutants. Artocarpus communis methanol extract (ACM) has many biological effects, such as antioxidant, anti-inflammatory, wound healing, and photoprotective effects; however, the poor water solubility of raw ACM has limited its applications in medicine and cosmetics. Topical antioxidant nanoparticles are one of the drug-delivery systems for overcoming the poor water solubility of antioxidants for increasing their skin penetration. The present study demonstrated that ACM-loaded hydroxypropyl-β-cyclodextrin and polyvinylpyrrolidone K30 nanoparticles (AHP) were successfully prepared and could effectively increase the skin penetration of ACM through changing the physicochemical characteristics of raw ACM, including reducing the particle size, increasing the surface area, and inducing amorphous transformation. Our results also revealed that AHP had significantly better antioxidant activity than raw ACM for preventing photocytotoxicity because the AHP formulation increased the cellular uptake of the ACM in UVB-irradiated HaCaT keratinocytes. In conclusion, our results suggest that AHP may be used as a good topical antioxidant nanoparticle for delivering ACM into deep layers of the skin for preventing UVB-induced skin problems.

Highlights

Artocarpus communis, which belongs to the family Moraceae, is a multi-purpose crop grown in southeast Asia and Taiwan
Raw A. communis methanol extract (ACM) can dissolve in organic solvents, such as alcohol and DMSO, but it is practically insoluble in water due to the poor water solubility of the index ingredient artocarpin that is abundant in ACM
These results indicate that HPBCD with polyvinylpyrrolidone K30 (PVPK30) co-carriers can be used to effectively encapsulate ACM into a nanoparticle system, and ACM-loaded PVPK30/HPBCD nanoparticles (AHP) at a ratio of 1:18:10 might be an optimal formulation with which to overcome the poor water solubility of raw ACM and for use in other experiments

Summary

Introduction

Artocarpus communis (synonym: Artocarpus altilis), which belongs to the family Moraceae, is a multi-purpose crop grown in southeast Asia and Taiwan. Its economic importance stems from its use in agriculture, folk medicine, and natural products. The ethnopharmacological uses of A. communis include the treatment of malarial fever, diarrhea, and infection. Previous studies have mentioned that A. communis methanol extract (ACM). Contains many phenolic compounds, including flavonoids, stilbenoids, arylbenzofurons, and jacalin [1], presenting many pharmacological activities, such as anti-inflammatory, antioxidant [2], wound healing [3], melanogenesis-inhibitory [4], and anti-cancer effects [5]. Raw ACM can dissolve in organic solvents, such as alcohol and DMSO, but it is practically insoluble in water due to the poor water solubility of the index ingredient artocarpin that is abundant in ACM. Organic solvents may cause several skin problems, Pharmaceutics 2021, 13, 1372.

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