Surface-Modified Bilosomes Nanogel Bearing a Natural Plant Alkaloid for Safe Management of Rheumatoid Arthritis Inflammation.

Mohammed H Elkomy,Naveed Ahmad,Ameeduzzafar Zafar,Hussein M Eid,Mohammed Elmowafy,Mohammed M Ghoneim,Essam M Eissa,Nabil K Alruwaili,Khaled Shalaby,Izzeddin Alsalahat

doi:10.3390/pharmaceutics14030563

Abstract

Rheumatoid arthritis (RA) is a chronic inflammatory illness affecting the joints. The characteristic of RA is gradual joint deterioration. Current RA treatment alleviates signs such as inflammation and pain and substantially slows the progression of the disease. In this study, we aimed to boost the transdermal delivery of berberine (a natural product) by encapsulating it in chitosan, surface-modified bilosomes nanogel for better management of the inflammation of RA. The chitosan-coated bilosomes loaded with berberine (BER-CTS-BLS) were formulated according to the thin-film hydration approach and optimized for various causal variables, considering the effect of lipid, sodium deoxycholate, and chitosan concentrations on the size of the particles, entrapment, and the surface charge. The optimized BER-CTS-BLS has 202.3 nm mean diameter, 83.8% entrapment, and 30.8 mV surface charge. The optimized BER-CTS-BLS exhibited a delayed-release profile in vitro and increased skin permeability ex vivo. Additionally, histological examination revealed that the formulated BLS had no irritating effects on the skin. Furthermore, the optimized BER-CTS-BLS ability to reduce inflammation was evaluated in rats with carrageenan-induced paw edema. Our results demonstrate that the group treated with topical BER-CTS-BLS gel exhibited a dramatic reduction in rat paw edema swelling percentage to reach 24.4% after 12 h, which was substantially lower than other groups. Collectively, chitosan-coated bilosomes containing berberine have emerged as a promising therapeutic approach to control RA inflammation.

Highlights

This article is an open access articleRheumatoid arthritis (RA) is a chronic inflammatory disease that affects about 0.5–1%of the global population and is marked by dysfunction in the immune system [1]
Initial experiments were conducted to determine the effect of various factors including sonication duration, hydration medium, lipid content, and drug concentration on BLS
BLS vesicles were prepared using Soybean Lecithin (SL) combined with cholesterol to boost vesicle entrapment and stability [47–49]

Summary

Introduction

This article is an open access articleRheumatoid arthritis (RA) is a chronic inflammatory disease that affects about 0.5–1%of the global population and is marked by dysfunction in the immune system [1]. Rheumatoid arthritis (RA) is a chronic inflammatory disease that affects about 0.5–1%. Signs such as edema, inflammation, and pain may occur. Pharmaceutics 2022, 14, 563 currently no cure for RA. Existing RA therapy alleviates symptoms, such as inflammation and discomfort, and slows down disease progression [3]. While current therapies for RA have demonstrated considerable effectiveness, 30% of the individuals who receive medication remain unresponsive to the first-line therapy. During a one-year treatment period, 30% of individuals acquire methotrexate intolerance due to serious side effects and systemic problems [4]. The development of novel natural medicines with enhanced therapeutic effectiveness and potential to provide aggregated and selective targeting of afflicted tissues is greatly on demand

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