Abstract
Lercanidipine has found to be effective in lowering blood pressure among the potent calcium channel blockers, through its action on L- type calcium channels. However, the major disadvantage associated with Lercanidipine is, it is a BCS class II drug having low solubility bioavailability is around 10% through oral route due of extensive first pass metabolism. The present study is aimed to prepare and evaluate polymeric nanoparticles of Lercanidipine using a combination of two bottom down techniques, High speed homogenizer and Probe sonication. Preformulation studies like, DSC, FTIR using surfactants such as Tween 80, Sodium Lauryl sulphate, Polyvinyl Alcohol, singely and in combination were used. A full factorial method was utilized to study the effect of various factors such as surfactant concentration, homogenization speed, sonication amplitude and sonication time on Lercanidipine nanoparticles in two levels. Optimized nanoparticles (with PVA as surfactant) showed an average particle size of 141 nm, PDI 0.248 and zeta potential +6.46. Formulation was further optimized using Design Expert 10 software. Optimized formulation was found to be stable during 3 months stability studies as per ICH guidelines.
Highlights
Hypertension is a silent invisible killer, which rarely causes symptoms [1]
A large number of conventional antihypertensive drugs are available in market but the major drawback with this route of drug delivery is low bioavailability, low solubility, substrates for p-glycoprotein enzymes (P-gp) and exhibit extensive high first pass metabolism
Technology to improve the solubility of drugs by reducing them to nano size ranges, increasing the surface area of the particle and improving the solubility by allowing greater contact with the surrounding dissolution medium. When such approach is extrapolated to polymers it is termed as a novel technology for drug delivery system in the form of polymeric nanoparticles
Summary
Hypertension is a silent invisible killer, which rarely causes symptoms [1]. It has led to stroke and heart diseases which is the leading cause of death in the world today [2]. A large number of conventional antihypertensive drugs are available in market but the major drawback with this route of drug delivery is low bioavailability, low solubility, substrates for p-glycoprotein enzymes (P-gp) and exhibit extensive high first pass metabolism. They have high dosing frequency and short half life. Technology to improve the solubility of drugs by reducing them to nano size ranges, increasing the surface area of the particle and improving the solubility by allowing greater contact with the surrounding dissolution medium When such approach is extrapolated to polymers it is termed as a novel technology for drug delivery system in the form of polymeric nanoparticles. In this study, polymeric nanoparticles of Lercanidipine have been prepared using a synthetic polymer aimed to enhance the solubility and bioavailability of Lercanidipine
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