Development and bioavailability assessment of ramipril nanoemulsion formulation.
The objective of our investigation was to design a thermodynamically stable and dilutable nanoemulsion formulation of Ramipril, with minimum surfactant concentration that could improve its solubility, stability and oral bioavailability. Formulations were taken from the o/w nanoemulsion region of phase diagrams, which were subjected to thermodynamic stability and dispersibility tests. The composition of optimized formulation was Sefsol 218 (20% w/w), Tween 80 (18% w/w), Carbitol (18% w/w) and standard buffer solution pH 5 (44% w/w) as oil, surfactant, cosurfactant and aqueous phase, respectively, containing 5 mg of ramipril showing drug release (95%), droplet size (80.9 nm), polydispersity (0.271), viscosity (10.68 cP), and infinite dilution capability. In vitro drug release of the nanoemulsion formulations was highly significant (p<0.01) as compared to marketed capsule formulation and drug suspension. The relative bioavailability of ramipril nanoemulsion to that of conventional capsule form was found to be 229.62% whereas to that of drug suspension was 539.49%. The present study revealed that ramipril nanoemulsion could be used as a liquid formulation for pediatric and geriatric patients and can be formulated as self-nanoemulsifying drug delivery system (SNEDDS) as a unit dosage form.
Shafiq
Sheikh
S
Department of Pharmaceutics, Jamia Hamdard, Hamdard Nagar, India. shafiq_sheikh@fastmail.fm
Shakeel
Faiyaz
F
Talegaonkar
Sushma
S
Ahmad
Farhan J
FJ
Khar
Roop K
RK
Ali
Mushir
M
D000284:Administration, Oral; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D001682:Biological Availability; D002021:Buffers; D002214:Capsules; D002626:Chemistry, Pharmaceutical; D004339:Drug Compounding; D004355:Drug Stability; D004655:Emulsions; D005026:Ethylene Glycols / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D008297:Male; D008954:Models, Biological; D053758:Nanoparticles; D009821:Oils / Q000737:chemistry*; D019999:Pharmaceutical Solutions; D044367:Phase Transition; D011136:Polysorbates / Q000737:chemistry; D017257:Ramipril / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods; D013816:Thermodynamics; D014783:Viscosity
D000806:Angiotensin-Converting Enzyme Inhibitors; D002021:Buffers; D002214:Capsules; D004655:Emulsions; D005026:Ethylene Glycols; D009821:Oils; D019999:Pharmaceutical Solutions; D011136:Polysorbates; D013501:Surface-Active Agents; C010111:carbitol; D017257:Ramipril