注射用PLGA阿德福韦微球;长期治疗慢性乙型肝炎的途径

StephenW

Eur J Pharm Sci. 2018 Mar 16. pii: S0928-0987(18)30131-3. doi: 10.1016/j.ejps.2018.03.016. [Epub ahead of print]
Injectable PLGA Adefovir microspheres; the way for long term therapy of chronic hepatitis-B.Ayoub MM1, Elantouny NG2, El-Nahas HM3, Ghazy FES3.
Author information
1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt. Electronic address: [email protected].2Department of Internal Medicine, Faculty of Medicine, Zagazig University, Zagazig, Egypt.3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt.

AbstractFor patient convenience, sustained release Adefovir Poly-d,l-lactic-co-glycolic acid (PLGA) microspheres were formulated to relieve the daily use of the drug which is a problem for patients treated from chronic hepatitis-B. PLGA microspheres were prepared and characterized by entrapment efficiency, particle size distribution and scanning electron microscopy (SEM). In-vitro release and in-vivo studies were carried out. Factors such as drug: polymer ratio, polymer viscosity and polymer lactide content were found to be important variables for the preparation of PLGA Adefovir microspheres. Fourier transform infrared (FTIR) analysis and differential scanning calorimetry (DSC) were performed to determine any drug-polymer interactions. One way analysis of variance (ANOVA) was employed to analyze the pharmacokinetic parameters after intramuscular injection of the pure drug and the selected PLGA microspheres into rats. FTIR and DSC revealed a significant interaction between the drug and the polymer. Reports of SEM before and after 1 and 24 h release showed that the microspheres had nonporous smooth surface even after 24 h release. The entrapment efficiency ranged between 55.83 and 86.95% and in-vitro release studies were continued for 16, 31 and 90 days. The pharmacokinetic parameters and statistical analysis showed a significant increase in the Tmax, AUC0-t and MRT, and a significant decrease in the Cmax of the tested formulation (p < 0.05). Results demonstrated that PLGA Adefovir microspheres could be used for long-term treatment of chronic hepatitis-B instead of the daily dose used by the patient.


KEYWORDS: Adefovir; Biodegradable microspheres; Entrapment efficiency; Poly-lactic-co-glycolic acid

PMID:29555501DOI:10.1016/j.ejps.2018.03.016

StephenW

Eur J Pharm Sci。 2018年3月16日。pii：S0928-0987（18）30131-3。 doi：10.1016 / j.ejps.2018.03.016。 [电子版提前打印]
注射用PLGA阿德福韦微球;长期治疗慢性乙型肝炎的途径。
Ayoub MM1，Elantouny NG2，El-Nahas HM3，Ghazy FES3。
作者信息

1
    埃及Zagazig Zagazig大学药剂学和工业药学系。电子地址：[email protected]。
2
    埃及Zagazig Zagazig大学医学院内科医学系。
3
    埃及Zagazig Zagazig大学药剂学和工业药学系。

抽象

为了方便患者，缓释阿德福韦聚-d，l-乳酸 - 乙醇酸共聚物（PLGA）微球被配制成缓解该药物的日常使用，这对于从慢性乙型肝炎治疗的患者是一个问题。制备PLGA微球并通过包封率，粒度分布和扫描电子显微镜（SEM）表征。进行体外释放和体内研究。发现药物：聚合物比例，聚合物粘度和聚合物丙交酯含量等因素是制备PLGA阿德福韦微球的重要变量。进行傅里叶变换红外（FTIR）分析和差示扫描量热法（DSC）以确定任何药物 - 聚合物相互作用。采用单因素方差分析（ANOVA）分析肌内注射纯药物和选定的PLGA微球后大鼠的药代动力学参数。 FTIR和DSC揭示了药物和聚合物之间的显着相互作用。在1和24小时释放之前和之后的SEM报告显示，甚至在释放24小时后，微球具有无孔光滑表面。包封率在55.83％和86.95％之间，体外释放研究持续16,31和90天。药代动力学参数和统计学分析显示T max，AUC 0-t和MRT显着增加，并且测试制剂的C max显着降低（p <0.05）。结果表明，PLGA阿德福韦微球可用于长期治疗慢性乙型肝炎，而不是患者使用的每日剂量。
关键词：

阿德福韦;生物可降解微球;包封效率;聚乳酸 - 共 - 乙醇酸

结论：
    29555501
DOI：
    10.1016 / j.ejps.2018.03.016

nevernevermind

这其实是个好方向：既然治愈如此之难而长期抗病毒一般都有效，拿考虑某种技术让抗病毒药物不用每天服用对病人来说也是某种解脱。
比如吃一片/打一针管半年。