Design, Development and Optimization of Ramipril Solid Lipid Nanoparticles Using Solvent Emulsification and Evaporation Method

Abstract

Background: Ramipril, an antihypertensive drug exhibits 28% of oral bioavailability and is also excreted out quickly through the kidneys. Moreover, numerous side effects of Ramipril have been reported such as, hypotension (postural), increasing potassium level, and angioedema, when it is presented as an immediate dosage form. Hence, to conquer the side-effects associated with the drug and to increase its bioavailability, the present study was undertaken. Objective: The objective of the proposed approach was to design, develop and optimize Ramiprilloaded solid lipid nanoparticles. Methods: Solvent emulsification and evaporation method were employed to prepare Ramiprilloaded solid lipid nanoparticles containing stearic acid and phosphatidylcholine as a lipid and surfactant, respectively. The prepared formulations were studied for particle size analysis, % entrapment efficiency, Zeta Potential, SEM, X-ray diffraction study, FTIR, NMR spectroscopy, in vitro release study and stability study. Result: The obtained results were noted to be within the standard limits. No interaction between Ramipril and other excipients, was confirmed with the FT-IR study of the formulations. Particle size analysis confirmed that the size of the prepared formulations ranged between 200-350 nm. The percent entrapment efficiency was observed in the range of 70.61-91.60%. The result of entrapment and particle size of the nanoparticles from the R5 batch was adjudged. The designed formulation noted a 70.50% cumulative drug release within a period of 7 h. The designed batch showed a mean zeta potential of -29.4 mV, exhibiting good stability of the formulation. Conclusion: The developed formulation was found to be stable and it represents a promising system for the sustained and controlled delivery of Ramipril.