Palmitic Acid–Pluronic F127–Palmitic Acid Pentablock Copolymer as a Novel Nanocarrier for Oral Delivery of Glipizide
Journal Title: Turkish Journal of Pharmaceutical Sciences - Year 2019, Vol 16, Issue 3
Abstract
Objectives: The aim of the present study was to develop nanotechnology-based oral formulations of glipizide to enhance the bioavailability and eliminate the frequent oral administration of the conventional dosage form. Glipizide is an antidiabetic drug with a short biological half-life and limited oral bioavailability. Novel palmitic acid–pluronic F127–palmitic acid (PA-F127) pentablock copolymer-based prolonged release glipizide nanoparticles (GNs) were prepared and screened for in vitro and in vivo studies. Materials and Methods: GNs were prepared using a novel PA-F127 pentablock copolymer by solvent evaporation technique. The prepared nanoparticles were evaluated for particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, percentage yield, and drug excipient compatibility using fourier transform infrared spectroscopy (FTIR) and differential scanning calorimeter (DSC) analysis, X-ray diffraction, scanning electron microscopy, in vitro drug release studies, stability studies, and in vivo pharmacokinetic studies. Results: The results of FTIR and DSC analysis revealed the absence of drug–excipient interactions. The optimized GN1 had particle size 242.60±4.20 nm, PDI 0.171±0.014, and zeta potential -21.41±0.462 mV. The prepared nanoparticles were spherical and showed semi-amorphous characteristics. The in vitro release studies showed 34.43±4.8% drug was released in the first 8 h and 56.11±4.12% glipizide was released further over 24 h. The GN1 was found to be stable at 5±3°C for up to 3 months. Pharmacokinetic studies showed that the orally administered GN1 was superior with Cmax 2.35-fold, tmax 1.6-fold, area under the curve (AUC0→∞) 3.3-fold, and mean residence time 1.2-fold as compared to pure glipizide (p<0.05). Conclusion: The bioavailability of the newly developed GN1 was successfully increased and the problem of frequent oral administration with the conventional dosage form can be overcome for diabetes treatment.
Authors and Affiliations
Vipan Kumar KAMBOJ, Prabhakar Kumar VERMA
Keywords
Related Articles
- EP ID EP48822
- DOI 10.4274/tjps.galenos.2018.20082
- Views 283
- Downloads 0
Effect of Extracts of the Aerial Parts and Roots from Four Ferulago Species on Erectile Dysfunction in Rats with Streptozotocin-Induced Diabetes
Objectives: The extracts of Ferulago species are used as aphrodisiacs in Turkey and so we aimed to demonstrate in vivo and in vitro the relaxant effect of four Ferulago species’ extracts on the corpus cavernosum (CC). M...
Global DNA Hypomethylation and Rassf1a and c-myc Promoter Hypermethylation in Rat Kidney Cells after Bisphenol A Exposure
Objectives: Bisphenol A (BPA) is a synthetic monomer used in the production of polycarbonate and an environmental contaminant with endocrine disrupting properties. BPA release from plastic carriers is thought to cause hi...
Knowledge and Attitudes Among Hospital Pharmacists About COVID-19
Objectives: Coronavirus (COVID-19) cases and deaths related to the virus have been reported all over the world. Pharmacists play an important role in conveying accurate information about COVID-19 to the community. The ai...
Development of Bioadhesive Buccal Tablets of Nicorandil Using a Factorial Approach
Objectives: In the present investigation, bioadhesive buccal tablets were prepared using the sustained-release polymer hydroxypropyl methylcellulose (HPMC) K100M, bioadhesive polymer neem gum, and an impervious backing l...
Effect of Medium pH and Light on Quinidine Production in Cinchona calisaya Wedd. Endophytic Fungi
Objectives: Quinidine has pharmaceutical importance as an antimalarial, antiarrhythmia, antimicrobial, anticancer, antioxidant, astringent, and bitter flavoring agent. Quinidine is in high demand, yet its production from...