Glimepiride-Loaded Nanoemulgel; Development, In Vitro Characterization, Ex Vivo Permeation and In Vivo Antidiabetic Evaluation

Abstract

Glimepiride (GMP), an oral hypoglycemic agent is extensively employed in the treatment of type 2 diabetes. Transdermal delivery of GMP has been widely investigated as a promising alternative to an oral approach but the delivery of GMP is hindered owing to its low solubility and permeation. The present study was designed to formulate topical nanoemulgel GMP system and previously reported solubility enhanced glimepiride (GMP/βCD/GEL-44/16) in combination with anti-diabetic oil to enhance the hypoglycemic effect. Nanoemulsions were developed using clove oil, Tween-80, and PEG-400 and were gelled using xanthan gum (3%, w/w) to achieve the final nanoemulgel formulations. All of the formulations were evaluated in terms of particle size, zeta potential, pH, conductivity, viscosity, and in vitro skin permeation studies. In vivo hypoglycemic activity of the optimized nanoemulgel formulations was evaluated using a streptozocin-induced diabetes model. It was found that a synergistic combination of GMP with clove oil improved the overall drug permeation across the skin membrane and the hypoglycemic activity of GMP. The results showed that GMP/βCD/GEL-44/16-loaded nanoemulgel enhanced the in vitro skin permeation and improved the hypoglycemic activity in comparison with pure and marketed GMP. It is suggested that topical nano emulsion-based GMP gel and GMP/βCD/GEL-44/16 could be an effective alternative for oral therapy in the treatment of diabetes.

Preparation, Characterization of Pregabalin and Withania coagulans Extract-Loaded Topical Gel and Their Comparative Effect on Burn Injury

“…The conductivity of all gels was in the order of drug- and extract-loaded nanogels (1111 µS/cm) > drug-loaded nanogels (632 µS/cm) > extract-loaded nanogel (221 µS/cm). The increase in conductivity is associated with an increase in water contents and more polar groups/polar nature of drug [ 27 ].…”

A Pharmaco-Technical Investigation of Thymoquinone and Peat-Sourced Fulvic Acid Nanoemulgel: A Combination Therapy

“…The formulation development and management of the stability of an NE critically rely on the successful screening of various excipients, such as oil, surfactants, and co-surfactants. Therefore, multiple oils such as kalonji, castor, olive, lavender, sunflower oil, and Capryol 90 (liquid lipid) were screened for the present formulation based on the drug solubility and miscibility [ 53 ]. The surfactants and co-surfactants considered for screening were Labrasol, PEG-200, PG, Tween 80, Tween 20, and Transcutol P based on their respective HLB values and ionic characteristics.…”

Polysaccharide-Based Transdermal Drug Delivery

“…The NE was prepared from clove oil, Tween-80, and PEG-400, gelated with XG. It improved skin permeability and hypoglycemic activity, providing a new option for the treatment of diabetes ( Figure 5 ) [ 129 ]. The ratio of polymer to surfactant has been proved to influence the permeation effect.…”

“… Schematic diagram of the preparation of the NE and its hypoglycemic effect, skin irritation, and in vivo antidiabetic evaluation [ 129 ]. Reproduced with permission from Fizza Abdul Razzaq, Cells; published by MDPI, 2021.…”