RESUMEN
This research work enhances the solubility, dissolution and bioavailability of Voriconazole which belongs to BCS II class. Carboxymethyl tamarind gum was synthesized by using carboxymethylation of tamarind gum. Solid dispersion of Voriconazole was developed by kneading method followed by immediate release tablets. Solid dispersion characterised for solubility and instrumental analysis. Tablets were evaluated for dissolution study. Solid dispersions were confirmed by presence of distinctive peaks at 1745.58 cm-1 (C=O) and 1402 cm-1 (-COO-), using Infrared spectroscopy. The weight loss of 3.91% and 54.42 % at 100°C and in the rage of 235°C-425°C respectively was observed. 13C nuclear magnetic resonance spectrum of carboxymethyl tamarind gum displayed three distinct peaks of C1, -OH, and CH2O- group. X-ray diffraction analysis confirmed that ccarboxymethyl tamarind gum exhibits an amorphous structure. Soild dispersion of Voriconazole were developed using the kneading method, incorporating carboxymethyl tamarind gum. Compared to traditional methods, Solid dispersion formulated with carboxymethyl tamarind gum demonstrated a significant increase in solubility enhancement, ranging from 68.12 to 74.37-fold. Notably, the SD5 formulation exhibited complete release from the solid dispersion within 120 minutes. In rat models, Voriconazole levels in the bloodstream were markedly elevated with the administration of solid dispersion. Furthermore, dissolution profiles of all formulation batches showed considerable improvement. These findings shed light on effective strategies for enhancing the dissolution and bioavailability of poorly soluble drugs, thus contributing to the advancement of drug delivery systems.
RESUMEN
The prolonged residence of drug formulation in the nasal cavity is of utmost importance for intranasal delivery of drug. Present investigation was aimed to develop a mucoadhesive in situ gel of Granisetron hydrochloride (GH) with reduced nasal mucocilliary clearance in order to improve the bioavailability of the antiemetic drug, granisetron hydrochloride. The in situ gelation upon contact with nasal mucosa was conferred via the use of the thermogelling Pluronic flake 127 (PF 127). Moringa gum (MG), carboxymethyl tamarind gum (CMTG) and sodium alginate (SA) was used to modulate mucoadhesion whereas drug release of optimized formulation was modified by 0.3% polyethylene glycol 6000 (PEG 6000). Results revealed that as the concentration of mucoadhesive polymer increased the mucoadhesive strength increased and gelation temperature decreased significantly. Preformulation studies showed that addition of GH in 18% PF 127 gels modulated gelation temperature significantly while mucoadhesive polymers alters mucoadhesion. Formulation F6, F11 and F15 showed more than 80% of drug diffusion at 240 min. Gelation temperature and mucoadhesive strength of all three formulations were found in the range of 30-31 C and 963.66±9.60 to 991.33±10.26 dyne/cm2 respectively. Formulation F11 showed optimum results and further histopathological evaluation reveled formulation is safe for use. Addition of PEG 6000 increased drug diffusion in formulation F11 with flux 0.034 mg.cm2/min. This study concluded the potential use of CMTG as mucoadhesive in situ nasal gel in terms of ease of administration, accuracy of dosing, prolonged nasal residence and improved nasal bioavailability.