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载有喷昔洛韦-薰衣草油纳米乳的口腔凝胶,可提高生物利用度并缓解唇疱疹相关疼痛。

Oral gel loaded with penciclovir-lavender oil nanoemulsion to enhance bioavailability and alleviate pain associated with herpes labialis.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia.

Center of Excellence for Drug Research and Pharmaceutical Industries, King Abdulaziz University, Jeddah, Saudi Arabia.

出版信息

Drug Deliv. 2021 Dec;28(1):1043-1054. doi: 10.1080/10717544.2021.1931561.

Abstract

Herpes labialis, caused by herpes simplex virus type 1, is usually characterized by painful skin or mucosal lesions. Penciclovir (PV) tablets are found to be effective against herpes labialis but suffer from poor oral bioavailability. This study aimed to combine the benefits of PV and lavender oil (LO), which exhibits anesthetic activity, in the form of a self-nanoemulsifying drug delivery system (SNEDDS) for the treatment of herpes labialis. Toward this purpose, LO (oil), Labrasol:Labrafil M1944 CS in the ratio of 6:4 (surfactant mixture), and Lauroglycol-FCC (co-surfactant, selected based on the solubility of PV) were evaluated as the independent factors using a distance quadratic mixture design. The formulation was optimized for the minimum globule size and maximum stability index and was determined to contain 14% LO, 40.5% Labrasol:Labrafil 1944 (6:4), and 45.5% Lauroglycol-FCC. The optimized PV-LO-SNEDDS was embedded in chitosan hydrogel and the resulting formulations coded by (O3) were prepared and evaluated. The rheological studies demonstrated a combined pseudoplastic and thixotropic behavior with the highest flux of PV permeation across sheep buccal mucosa. Compared to a marketed 1% PV cream, the O3 formulation exhibited a significantly higher and sustained PV release, nearly twice the PV permeability, and a relative bioavailability of 180%. Overall, results confirm that the O3 formulation can provide an efficient delivery system for PV to reach oral mucosa and subsequent prolonged PV release. Thus, the PV-LO-SNEDDS embedded oral gel is promising and can be further evaluated in clinical settings to establish its therapeutic use in herpes labialis.

摘要

唇疱疹由单纯疱疹病毒 1 型引起,通常表现为疼痛的皮肤或黏膜损伤。喷昔洛韦(PV)片剂被发现对唇疱疹有效,但口服生物利用度差。本研究旨在将 PV 和薰衣草油(LO)的优势结合在一起,LO 具有麻醉活性,以自微乳给药系统(SNEDDS)的形式治疗唇疱疹。为此,LO(油)、Labrasol:Labrafil M1944 CS(表面活性剂混合物)的比例为 6:4,以及 Lauroglycol-FCC(根据 PV 的溶解度选择的助表面活性剂)被评估为独立因素,采用距离二次混合物设计。该配方优化了最小液滴尺寸和最大稳定性指数,确定含有 14%的 LO、40.5%的 Labrasol:Labrafil 1944(6:4)和 45.5%的 Lauroglycol-FCC。优化后的 PV-LO-SNEDDS 被嵌入壳聚糖水凝胶中,并制备和评估了由此产生的编码为(O3)的制剂。流变学研究表明具有假塑性和触变性的组合行为,并且 PV 穿过绵羊颊黏膜的通量最高。与市售的 1%PV 乳膏相比,O3 制剂表现出显著更高和持续的 PV 释放,PV 渗透率几乎增加了一倍,相对生物利用度为 180%。总体而言,结果证实 O3 制剂可为 PV 到达口腔黏膜并随后延长 PV 释放提供有效的给药系统。因此,嵌入 PV-LO-SNEDDS 的口腔凝胶具有很大的应用前景,可以在临床环境中进一步评估,以确定其在唇疱疹中的治疗用途。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/97eb/8175053/e0cd93e61bdf/IDRD_A_1931561_F0001_C.jpg

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