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ISSN 2063-5346
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FORMULATION, OPTIMIZATION AND CHARACTERIZATION OF TICAGRELOR-LOADED SOLID LIPID NANOPARTICLES USING CENTRAL COMPOSITE DESIGN

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Shailaja Pashikanti, Aswini Lavanya Pudi, Dinesh Kumar Chandanapalli
» doi: 10.48047/ecb/2023.12.7.305

Abstract

Ticagrelor (TGL) is an antiplatelet agent that belongs to BCS class IV and has an oral bioavailability of 36%. Objectives: The intention of my present study is to develop an optimized formulation of Solid lipid nanoparticles that increase the solubility and permeability of ticagrelor by using a central composite design. Materials and methods: The PSLNs are prepared using the hot homogenization method, GMS, Poloxamer407 and Tween 80. The lipid to drug ratio (X1), the concentration of surfactant (X2) and the amount of PEG 2000 (X3) are considered as independent variables and particle size, Zeta potential, % Encapsulation efficiency and PDI are considered as the dependent variables. The optimized PSLNs are further characterized for an in-vitro, ex vivo, DSC, SEM and TEM analysis. Results: Initial trail runs are done for selecting the ranges for optimization. The design provided 16 runs, the particle size, zeta potential, %EE and PDI ranges from 323nm to 648nm; -21.45mV to -37.63mV; 83.28% to 92.00% and 0.42 to 0.52 respectively. The optimized formulation developed from the design with 0.548 probability showed 468.9nm particle size, -29.37mV zeta-potential, 88.87% EE and 0.36 PDI. This showed in-vitro release up to 24h with 93.42% drug release and it showed non-fickian diffusion as the n value is 0.52. The ex-vivo has a steady-state flux of 0.0096mg/cm2 min The SEM and TEM studies showed that the formulation was pegylated and the drug was encapsulated.

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