Intravenous delivery of furosemide using lipid-based versus polymer-based nanocapsules: in vitro and in vivo studies

被引:2
作者
Kamel, Yasmine N. [1 ]
El-Marakby, Eman M. [2 ]
Gad, Heba A. [2 ,3 ]
机构
[1] CID Co Chem & drug Ind, Giza, Egypt
[2] Ain Shams Univ, Fac Pharm, Dept Pharmaceut & Ind Pharm, Cairo 11566, Egypt
[3] Batterjee Med Coll, Dept Pharmaceut Sci, Pharm Program, Jeddah, Saudi Arabia
关键词
Furosemide; lipid nanocapsules; polymeric nanocapsules; hypertension; cardiac failure; sterilization; EX-VIVO; CORE NANOCAPSULES; LOOP DIURETICS; HEART-FAILURE; DRUG-RELEASE; NANOPARTICLES; OPTIMIZATION; HEMOCOMPATIBILITY; PHARMACOKINETICS; ENCAPSULATION;
D O I
10.1080/10837450.2024.2389855
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Objectives: Furosemide (FSM), a potent loop diuretic, is used to treat edema due to hypertension, congestive heart failure, and liver and renal failures. FSM applications are limited by its low bioavailability. Our aim is to use different nanoencapsulation strategies to control the release of FSM and enhance its pharmacokinetic properties. Methods: Two types of FSM-loaded nanocapsules, namely FSM-loaded lipid nanocapsules (LNCs) and polymeric nanocapsules (PNCs), were developed, physicochemically characterized, and subjected to pharmacokinetic and pharmacodynamic studies. Lipid nanocapsules were prepared by the simple phase inversion method using Labrafac (TM) lipid, while the polymeric nanocapsules were prepared by nanoprecipitation method using polycaprolactone polymer. Results: Transmission electron microscopy ascertains spherical structures, corroborating the nanometric diameter of both types of nanocapsules. The particle size of the optimized FSM-loaded LNCs and FSM-loaded PNCs was 32.19 +/- 0.72 nm and 230.7 +/- 5.13 nm, respectively. The percent entrapment efficiency was 63.56 +/- 1.40% of FSM for the optimized PNCs. The in vitro release study indicated prolonged drug release compared to drug solutions. The two loaded nanocapsules systems succeeded in enhancing the pharmacokinetic parameters in comparison to the marketed FSM solution with superior diuretic activity (p < 0.05). The results of the stability study and the terminal sterilization by autoclave indicated the superiority of LNCs over PNCs in maintaining the physical parameters under storage conditions and the drastic conditions of sterilization. Conclusions: LNCs and PNCs are considered promising nanosysems for improving the diuretic effect of FSM.
引用
收藏
页码:738 / 750
页数:13
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