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拟薄水铝石作为阿昔洛韦的药物递送系统。

Pseudoboehmite as a drug delivery system for acyclovir.

作者信息

Peres Renato Meneghetti, Sousa Jéssica Maiara Leme, de Oliveira Mariana Oliva, Rossi Maura Vincenza, de Oliveira Rene Ramos, de Lima Nelson Batista, Bernussi Ayrton, Warzywoda Juliusz, Sarmento Bruno, Munhoz Antonio Hortencio

机构信息

School of Engineering, Mackenzie Presbyterian University, Rua da Consolação, 930, Building 33, Consolação, São Paulo, SP, 01302-907, Brazil.

CCBS, Mackenzie Presbyterian University, São Paulo, Brazil.

出版信息

Sci Rep. 2021 Jul 29;11(1):15448. doi: 10.1038/s41598-021-94325-y.

Abstract

Herpes simplex virus is among the most prevalent sexually transmitted infections. Acyclovir is a potent, selective inhibitor of herpes viruses and it is indicated for the treatment and management of recurrent cold sores on the lips and face, genital herpes, among other diseases. The problem of the oral bioavailability of acyclovir is limited because of the low permeability across the gastrointestinal membrane. The use of nanoparticles of pseudoboehmite as a drug delivery system in vitro assays is a promising approach to further the permeability of acyclovir release. Here we report the synthesis of high purity pseudoboehmite from aluminium nitrate and ammonium hydroxide containing nanoparticles, using the sol-gel method, as a drug delivery system to improve the systemic bioavailability of acyclovir. The presence of pseudoboehmite nanoparticles were verified by infrared spectroscopy, transmission electron microscopy, and X-ray diffraction techniques. In vivo tests were performed with Wistar rats to compare the release of acyclovir, with and without the addition of pseudoboehmite. The administration of acyclovir with the addition of pseudoboehmite increased the drug content by 4.6 times in the plasma of Wistar rats after 4 h administration. We determined that the toxicity of pseudoboehmite is low up to 10 mg/mL, in gel and the dried pseudoboehmite nanoparticles.

摘要

单纯疱疹病毒是最常见的性传播感染之一。阿昔洛韦是一种强效、选择性的疱疹病毒抑制剂,适用于治疗和管理嘴唇和面部复发性唇疱疹、生殖器疱疹等疾病。由于阿昔洛韦跨胃肠膜的渗透性低,其口服生物利用度存在问题。在体外试验中使用拟薄水铝石纳米颗粒作为药物递送系统是提高阿昔洛韦释放渗透性的一种有前景的方法。在此,我们报告了使用溶胶-凝胶法从含纳米颗粒的硝酸铝和氢氧化铵合成高纯度拟薄水铝石,作为一种药物递送系统以提高阿昔洛韦的全身生物利用度。通过红外光谱、透射电子显微镜和X射线衍射技术验证了拟薄水铝石纳米颗粒的存在。用Wistar大鼠进行体内试验,比较添加和不添加拟薄水铝石时阿昔洛韦的释放情况。给药4小时后,添加拟薄水铝石的阿昔洛韦给药使Wistar大鼠血浆中的药物含量增加了4.6倍。我们确定,在凝胶和干燥的拟薄水铝石纳米颗粒中,拟薄水铝石在浓度高达10mg/mL时毒性较低。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6166/8322319/af6ca61fb373/41598_2021_94325_Fig1_HTML.jpg

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