| Abstrakt: |
Nateglinide (NTG) belongs to the meglitinide class, an oral hypoglycemic agent used in the treatment of insulin-resistant (Type II) diabetes mellitus. Potential constraints associated with NTG delivery include poor aqueous solubility, short action time, and quick elimination, which causes variable bioavailability. Therefore, the present study aimed to develop and optimize nanostructured lipid carriers (NLCs) formulation to improve the oral bioavailability of NTG for the effective treatment of diabetes. NLCs were prepared by a modified HPH method using a Box–Behnken design (BBD) approach. Glyceryl monostearate, Miglyol 812, and Acrysol EL 135 were chosen as solid lipid, liquid lipid, and surfactant, respectively. Obtained NLCs were characterized for physicochemical properties, in vitro drug release studies, and pharmacokinetic parameters. NTG-NLCs exhibited small particle size ranging from 142.8 ± 1.67 to 252.7 ± 2.17 nm zeta potential ranging from 13.53 to 30.93 mV; Polydispersibility Index (PI) was ranging from 0.343 ± 0.071 to 0.417 ± 0.058. The average encapsulation efficiency for the NLCs was 89.99%. Optimized NTG-NLC showed particle size of 142.8 nm, zeta potential of + 30.93 mV, drug loading of 16.04%, and entrapment efficiency of 93.48%. In a pharmacokinetic study, the relative oral bioavailability of NTG-NLC was increased by 3.77 times that of pure NTG and 1.54 times that of Glinate 60 marketed NTG formulation. The half-life of the drug was prolonged by 1.6 times. The solubility and bioavailability of NTG were enhanced, coupled with its prolonged release. NTG-NLC prepared by the modified HPH method is a promising technique to enhance in vitro drug release, bioavailability, and pharmacokinetics. [ABSTRACT FROM AUTHOR] |
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