Design and Optimization of Pioglitazone Hydrochloride Self-Nanoemulsifying Drug Delivery System (SNEDDS) Incorporated into an Orally Disintegrating Tablet

Abstract

Pioglitazone Hydrochloride (PGZ) suffers from poor aqueous solubility. The aim of this research was to design orally disintegrating tablets with self-nanoemulsifying properties (T-SNEDDS) to improve the Pioglitazone solubility and dissolution rate. Three liquid self-nanoemulsifying systems (L-SNEDDS) were formulated and evaluated for transmittance percentage, emulsification time, particle size, Poly dispersity index (PDI), percentage of content, solubility and stability. The optimum L-SNEDDS formula was converted to a solidified self-nanoemulsifying drug delivery system (S-SNEDDS) by adsorption on Syloid (SYL). Powder characterization tests, such as flowability tests, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD) and scanning electron microscopy (SEM), were performed for the selected S-SNEDDS formulation. Orally disintegrating tablets (ODT) were formulated by blending S-SNEDDS with tableting excipients. The ODT tablet batch composed of Prosolv was selected for tablet quality control tests, such as hardness, friability, disintegration time, content uniformity, weight variation, in vitro release, in vivo studies and accelerated stability studies. ODT tablets showed accepted mechanical properties and rapid disintegration time (<30 s). No drug degradation was observed at 3 months into the accelerated stability study. The optimized L-SNEDDS, S-SNEDDS and ODT (T-SNEDDS), showed significant enhancement of PGZ in vitro dissolution profiles compared to the pure drug (p > 0.05). In vivo pharmacokinetic and pharmacodynamic evaluation of ODTs showed better behavior compared to the raw drug suspension and the commercial tablet (p > 0.05). Orally disintegrating tablets revealed a promising potential to improve Pioglitazone poor aqueous solubility, dissolution profile and bioavailability.

Isotretinoin self-nano-emulsifying drug delivery system: Preparation, optimization and antibacterial evaluation

“…Emulsification time ranged from 10 − 40 sec for the tested formulations. It was observed that rapid emulsification was contributed to formulations with low oil content of 10–20 % w/w and high cosurfactant content 50–70 % w/w that produce mixtures of low viscosities ( Teail, 2022 ).…”

Development and Optimization of Nigella sativa Nanoemulsion Loaded with Pioglitazone for Hypoglycemic Effect

“…A quantity of 100 µL of optimized PGZ -loaded NE formulation was diluted in 25 mL methanol and vortexed for 3 min using a vortex mixer (VELP Scintifica, Usmate Velate, Italy). The drug content was evaluated spectrophotometrically using a UV spectrophotometer (JENWAY 6305, Bibby Scientific Ltd., Staffs, UK) at λ max 269 nm [ 7 ]. An identical technique was used for the blank NE (sample without drug).…”

“…Its capacity for the improved control of blood glucose level and lipid profile has been established, along with demonstration of tolerable side-effects [ 6 ]. However, according to its categorization in the Biopharmaceutical Classification System (BCS), it is characterized as a class II drug, which exhibits poor solubility and high permeability [ 7 ]. This presents a challenge for PGZ formulation as it necessitates the development of a dosage form that can incorporate a drug with low solubility in water.…”

Design, Optimization and Characterization of Self-Nanoemulsifying Drug Delivery Systems of Bilastine

“…The USP dissolving equipment, Type II, was used for the in-vitro drug released test, which was carried out at 37 °C with a 100-rpm rotation speed, moreover, the dissolving medium was 300 mL of 0.1N HCl. The dialysis bag was employed to gather the amount of truly free BL without interference of unreleased drug from nanoemulsion (20) . Before the in-vitro release study began, dialysis bags (Mwt cut off 8,000-14,000 Daltons) were soaked for 24 hours at room temperature in freshly prepared 0.1N HCl (21) .…”