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异维 A 酸纳米胶体载体:对痤疮丙酸杆菌的抗菌活性和皮肤动力学建模。

Nanocolloidal carriers of isotretinoin: antimicrobial activity against Propionibacterium acnes and dermatokinetic modeling.

机构信息

UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles and Nanocomposites, Panjab University, Chandigarh, India.

出版信息

Mol Pharm. 2013 May 6;10(5):1958-63. doi: 10.1021/mp300722f. Epub 2013 Apr 12.

DOI:10.1021/mp300722f
PMID:23544848
Abstract

Acne, a common skin disease in teenagers, is caused by Propionibacterium acnes (P. acnes). Isotretinoin (ITR) is though reported to have immense antiacne potential, yet there are hardly any reports vouching its antimicrobial activity. The present study, therefore, was undertaken to study the antimicrobial activity of ITR and evaluate the effect of its encasement in nanocarriers on its minimum inhibitory concentration (MIC). The nanocarriers were also evaluated for the skin transport characteristics. MICs of pure drug and entrapped drug in nanolipid carriers (ITR-NLCs) and in solid lipid nanoparticles (ITR-SLNs) were determined by broth dilution method against clindamycin phosphate as the reference antibiotic. It was observed that ITR possessed marked antimicrobial activity against anaerobic pathogen, P. acnes. Nanocarriers loaded with ITR, that is, SLNs and NLCs, enhanced the antimicrobial activity even at lower concentrations vis-à-vis the drug alone and improved drug transport potential vis-à-vis the commercial gel. The unique findings could be the result of effective adhesion of ITR-loaded nanocarriers to the bacterial membranes and release of drug directly to the target. Besides establishing ITR as an antimicrobial agent against acne-causing bacteria, the current work ratifies immense potential of nanocolloidal carriers like SLNs and NLCs to treat acne in a more efficient manner.

摘要

痤疮是青少年中常见的皮肤病,由痤疮丙酸杆菌(P. acnes)引起。异维 A 酸(ITR)虽然被报道具有巨大的抗痤疮潜力,但几乎没有任何报道证明其具有抗菌活性。因此,本研究旨在研究 ITR 的抗菌活性,并评估其在纳米载体中的包封对最小抑菌浓度(MIC)的影响。还评估了纳米载体的皮肤传输特性。通过肉汤稀释法测定纯药物和纳米脂质载体(ITR-NLCs)和固体脂质纳米粒(ITR-SLNs)中包封药物的 MIC,以磷酸克林霉素作为参考抗生素。结果表明,ITR 对厌氧病原体痤疮丙酸杆菌具有明显的抗菌活性。载有 ITR 的纳米载体,即 SLNs 和 NLCs,即使在较低浓度下也能增强抗菌活性,与单独使用药物相比,提高了药物传输潜力,与商业凝胶相比。这一独特的发现可能是由于 ITR 负载的纳米载体有效地粘附在细菌膜上,并将药物直接释放到靶标上。除了确立 ITR 作为一种对抗痤疮细菌的抗菌剂外,目前的工作还证实了像 SLNs 和 NLCs 这样的纳米胶体载体具有巨大的潜力,可以更有效地治疗痤疮。

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