Abstract
Objective: The aim was to formulate and evaluate self-nanoemulsifying drug delivery systems (SNEDDS) of ramipril, an antihypertensive drug to improve the solubility and bioavailability.
 Methods: Based on solubility studies oil phase (Sefsol 218), surfactant (Acrysol EL135), and cosurfactant (Transcutol P), respectively, were selected to prepare SNEDDS. Ramipril SNEDDS optimized employing box-Behnken design through the study of factors. All formulations were evaluated for particle size, zeta potential (ZP), polydispersity index (PDI), entrapment efficiency (EE), drug content, and in vitro drug release. The optimized formulation was characterized for Fourier transform infrared (FTIR), scanning electron microscopy (SEM), stability studies, and pharmacokinetic study.
 Results: The mean particle size, PDI, ZP, EE, content uniformity, and in vitro drug release profile of optimized ramipril-loaded SNEDDS (RF14) were found to be 75.3±2.21nm, 0.126±0.05, −24.4±5.78mV, 98.74±1.97%, 99.52±1.67%, and 98.65±1.73%, respectively. FTIR studies revealed that there is no incompatibility between drug and excipients, SEM images exhibited nanoparticles to be more porous and in spherical shape. Stability studies indicated formulation was stable for 6 months. In vivo studies were conducted for optimized formulation RF14, the Tmax was found to be 0.5±0.62 and 0.5±0.95 h for the optimized and commercial formulations respectively, while Cmax was 25.16±1.73 ng/mL was significant (p<0.05) as compared to the ramipril pure drug 8.02±0.086 ng/mL. AUC0-t of the SNEDDS formulation was higher 355.49±1.76ng h/ml compared to pure drug 116.57±1.64 ng h/ml indicated higher amount of drug concentration in blood proving better systemic absorption of ramipril from SNEDDS formulation as compared to the pure drug.
 Conclusion: It is concluded from the results that ramipril was successfully formulated into SNEDDS with higher concentration with fast action.
Highlights
The Class II to Class IV drugs of biopharmaceutical classification system suffering with poor water solubility led to the lower intestinal absorption and lower bioavailability
Percentage drug content and EE The % drug content of all ramipril Self-nanoemulsifying drug delivery systems (SNEDDS) ranged from 95.13±1.17 to 99.52±1.67% and the EE varied between 94.35±1.62 and 98.74±1.97% with maximum value recorded for RF14
Polydispersity index (PDI) The polydispersity index (PDI) of all SNEDDSs was significantly varying from 0.126 to 0.158 to as depicted in Table 3 indicating narrow size distribution which reveals the higher stability of Ramipril solid lipid nanoparticles [15]
Summary
The Class II to Class IV drugs of biopharmaceutical classification system suffering with poor water solubility led to the lower intestinal absorption and lower bioavailability. Lipid-based drug formulations increase the relative solubility of drugs in GI track by enhancing absorption. Self-nanoemulsifying drug delivery systems (SNEDDS) lipid-based formulations are most promising technology in drug delivery [1]. SNEDDS formulation is used for increasing the solubility, oral bioavailability, and permeability of drug. It protects the drug from hostile environment in GI track and is used for selective GI targeting drug delivery [2]. They have particle size ranging from nanometers to few microns.
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