1*School of Pharmacy, Lingaya's Vidyapeeth (A Deemed-to-be-University), Nachauli, Jasana Road, Faridabad, Haryana, India. E-mail: nagamohit00@gmail.com
2School of Pharmacy, Lingaya's Vidyapeeth (A Deemed-to-be-University), Nachauli, Jasana Road, Faridabad, Haryana, India.
3R. V. Northland Institute of Pharmacy, Dadri, G. B. Nagar, Uttar Pradesh, India.
Corresponding author: Mohit Nagar, Research Scholar, School of Pharmacy, Lingaya's Vidyapeeth (A Deemed-to-be-University), Nachauli, Jasana Road, Faridabad, Haryana, India. Email: nagamohit00@gmail.com
Diabetes mellitus is a persistent endocrine disorder in which impaired insulin secretion or action leads to elevated circulating glucose levels. Charantin, a major antidiabetic phytoconstituent of Momordica charantia, exhibits strong hypoglycemic activity but is limited aqueous solubility and low oral bioavailability. This study aimed to development, formulate and evaluate charantin-loaded polymeric nanoparticles incorporated into a topical nanogel to enhance topical delivery and antidiabetic efficacy. Polymeric nanoparticles were formulated by ionic gelation and optimized for desirable physicochemical properties. The optimized polymeric nanoparticle formulation (CRT-2A) showed a particle droplet size-200±03 nm, PDI- 0.053±00.3, and zeta potential –24.0± 1.4 mV, indicating uniformity and stability. Encapsulation efficiency was 88.4 ± 2.7%, drug loading 31.84 ± 0.61%, with 92% in-vitro release and 88.92% ex-vivo permeation over 24 hours. Optimized formulation (CRT-2A) was integrated into a 1% Carbopol 938 solution and convert into nanogel (CRT-NG) exhibiting suitable pH (6.7 ± 0.1), viscosity (12,423 ± 75 cps), good spread-ability (10.30 ± 0.8 g·cm/s), and smooth homogeneity, indicating excellent consistency, suitability and ideal used for topical delivery. The optimized formulation (CRT-NG) exhibited First-order release kinetics with a diffusion-controlled mechanism, and ex-vivo studies showed a 2.86-fold enhancement in skin permeation compared to the pure charantin gel. In STZ-induced diabetic rats, CRT-NG (25 and 50 mg/kg) significantly improved glycemic control and glucose tolerance compared to diabetic controls (p < 0.05). High and low-dose of drug loaded nanogel treatments showed antidiabetic effects of comparable to metformin. Overall, charantin-loaded polymeric nanoparticle topical nanogel showed enhanced skin permeation, sustained drug release, and improved antidiabetic efficacy, highlighting its potential as a promising transdermal delivery system for effective diabetes management.
Keywords: Polymeric Nanoparticle, Charantin, Diabetes Mellitus, STZ-induced rats, Topical Gel, Antidiabetic Activity.
Figure: Schematic outline of formulation and in vivo evaluation.
How to cite this article: Mohit Nagar, Ajay Pal Singh, Sanjar Alam. Formulation, Optimization, Characterization, and In Vivo Antidiabetic Evaluation of Bioactive Loaded Polymeric Nanoparticles Incorporated into Topical Nanogel in STZ-Induced Diabetic Rats. Int J Drug Deliv Technol. 2026; 16(8s): 504-517; DOI: 10.25258/ijddt.16.8s.62
Source of support: Nil.
Conflict of interest: None