Sustained release of Ambrisentan solid lipid nanoparticles for the treatment of hypertension: Melt emulsification method.

Abstract

Objective: The beneficial usefulness is limited because of its deprived solubility and bioavailability. The recent work deals with the advancement of solid lipid nanoparticles of Ambrisentan for the effective therapy of pulmonary hypertension intended for oral delivery.

Material and methods: The solid lipid nanoparticles of Ambrisentan were developed using the melt emulsification method. The characterization of Ambrisentan was carried out with FTIR, DSC, and crystalline nature with XRD. The optimization was accomplished with the Box-Behnken design. The glyceryl monostearate (GMS), Tween 80, and sonication time were considered independent factors and the particle size, and entrapment efficiency were the critical quality attributes in the development of SLN.

Results: The compatibility, thermal nature, and crystalline behavior were confirmed with FTIR, DSC, and XRD respectively. The preferred batch F10 indicated a particle size of 166.7nm and an entrapment efficiency of 83.96%. The cumulative percentage of drug dissolved from the optimized Ambrisentan-loaded SLN was 87.68% after 24h indicating a sustained release pattern. Furthermore, after lyophilization and estimated with scanning electron microscopy a particle size of 153.5 to 179.8nm was confirmed. The lyophilized powder is intended for oral delivery and has significant bioavailability, minimizing the chances of mortality due to its sustained release action.

Conclusion: The significant improvement in solubility of Ambrisentan was achieved through solid lipid nanoparticles which facilitates greater efficacy.