Non-invasive caffeinated-nanovesicles as adipocytes-targeted therapy for cellulite and localized fats

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Lobna M. Khalil , Wessam M. El-Refaie , Yosra S.R. Elnaggar , Hamdy Abdelkader , Adel Al Fatease , Ossama Y. Abdallah
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Abstract

Caffeine (CAF) is a non-selective adenosine A1 receptor antagonist which predominates in fat cells. When CAF binds to adenosine receptors, it increases cyclic adenosine monophosphate; inhibiting adipogenesis and inducing fat lipolysis. Resveratrol (RSV) is an antioxidant polyphenol possessing different anti-obesity mechanisms. Topical application of both hydrophilic CAF and lipophilic RSV is limited.

This study aimed to develop novel caffeinated-resveratrol bilosomes (CRB) and caffeine-bilosomes (CB) that could non-invasively target and deposit in fat cells. RSV bilosomes (RB) were prepared as a non-targeted system for comparison. CRB showed nanosize (364.1 nm ±6.5 nm) and high entrapment for both active compounds. Rats treated topically with CRB revealed a significant decrease (P = 0.039) in body weight. Histological analysis of the excised skin demonstrated a reduction in the subcutaneous fatty layer thickness and a decrease in the size of connective tissue-imbedded fat cells. Kidney histological examination of RB-treated rats showed subcapsular tubular epithelial cells with cytoplasmic vacuolation. This reflects a systemic effect of RSV from the non-targeted RB compared to CRB, which had a targeting effect on the adipose tissue. In conclusion, CAF in CRB significantly enhanced RSV deposition in adipose tissue and assisted its local-acting effect for managing obesity and cellulite.

Abstract Image

无创咖啡因纳米囊泡作为脂肪细胞靶向疗法治疗橘皮组织和局部脂肪
咖啡因(CAF)是一种非选择性腺苷 A1 受体拮抗剂,在脂肪细胞中占主导地位。当 CAF 与腺苷受体结合时,它会增加单磷酸环腺苷;抑制脂肪生成并诱导脂肪分解。白藜芦醇(RSV)是一种抗氧化多酚,具有不同的抗肥胖机制。本研究旨在开发新型咖啡因白藜芦醇双糖体(CRB)和咖啡因双糖体(CB),它们可以非侵入性地靶向沉积在脂肪细胞中。此外,还制备了 RSV 双糖体(RB)作为非靶向系统进行比较。CRB显示出纳米级尺寸(364.1 nm ±6.5 nm),对两种活性化合物都有很高的吸附性。大鼠经 CRB 局部治疗后体重显著下降(P = 0.039)。切除皮肤的组织学分析表明,皮下脂肪层厚度减少,结缔组织包裹的脂肪细胞体积缩小。经 RB 处理的大鼠的肾脏组织学检查显示,肾小管上皮细胞有胞浆空泡。这反映了 RSV 对非靶向 RB 的全身影响,而对脂肪组织有靶向作用的 CRB 则没有这种影响。总之,CRB 中的 CAF 能显著增强 RSV 在脂肪组织中的沉积,并增强其局部作用效果,从而控制肥胖和橘皮组织。
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来源期刊
International Journal of Pharmaceutics: X
International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.60
自引率
0.00%
发文量
32
审稿时长
24 days
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