FORMULATION AND DEVELOPMENT OF VORICONAZOLE TABLETS CONTAINING SOLID DISPERSION WITH ENHANCED SOLUBILITY, DISSOLUTION AND BIOAVAILABILITY
DOI:
https://doi.org/10.25004/IJPSDR.2024.160212Keywords:
Voriconazole, tamarind gum, solid dispersion, carboxymethylated tamarind gum, bioavailability, solubilityAbstract
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.
Downloads
References
Peyton LR, Gallagher S, Hashemzadeh M. Triazole antifungals: a review. Drugs Today. 2015; 51(12):705-718.
Soe HM, Kerdpol K, Rungrotmongkol T, Pruksakorn P, Autthateinchai R, Wet-Osot S, Loftsson T, Jansook P. Voriconazole Eye Drops: Enhanced Solubility and Stability through Ternary Voriconazole/Sulfobutyl Ether β-Cyclodextrin/Polyvinyl Alcohol Complexes. Int. J. Mol. Sci. 2023; 24(3):2343.
Pawar SR, Barhate SD. Solubility enhancement (Solid Dispersions) novel boon to increase bioavailability. J. drug deliv. ther. 2019; 9(2):583-590.
Teixeira-Costa BE, Andrade CT. Natural polymers used in edible food packaging—History, function and application trends as a sustainable alternative to synthetic plastic. Polysaccharides. 2022; 3(1):32-58.
Idrees H, Zaidi SZ, Sabir A, Khan RU, Zhang X, Hassan SU. A review of biodegradable natural polymer-based nanoparticles for drug delivery applications. Nanomaterials. 2020; 10(10):1970.
Malviya R, Sundram S, Fuloria S, Subramaniyan V, Sathasivam KV, Azad AK, Sekar M, Kumar DH, Chakravarthi S, Porwal O, Meenakshi DU. Evaluation and Characterization of Tamarind Gum Polysaccharide: The Biopolymer. Polymers. 2021;13(18):3023.
Yamatoya K, Tabuchi A, Suzuki Y, Yamada H. Tamarind seed polysaccharide: unique profile of properties and applications. Biopolymer-Based Formulations. 2020; 445-461.
Shukla AK, Bishnoi RS, Kumar M, Fenin V, Jain CP. Applications of tamarind seeds polysaccharide-based copolymers in controlled drug delivery: An overview. Asian J. Pharm. Pharmacol. 2018; 4:23-30.
Kumar CS, Bhattacharya S. Tamarind seed: properties, processing and utilization. Crit. Rev. Food Sci. Nutr. 2008; 48(1):1-20.
Nayak AK, Pal D. Functionalization of tamarind gum for drug delivery. Funct. biopolym. 2018; 25-56.
Warkar SG. Potential applications and various aspects of polyfunctional macromolecule-carboxymethyl tamarind kernel gum. Eur. Polym. J. 2020; 140:110042.
Badwaik HR, Kumari L, Maiti S, Sakure K, Nakhate KT, Tiwari V, Giri TK. 2022. A review on challenges and issues with carboxymethylation of natural gums: The widely used excipients for conventional and novel dosage forms. Int. J. Biol. Macromol. 2022;11-15.
Goyal P, Kumar V, Sharma P. 2007. Carboxymethylation of tamarind kernel powder. Carbohydr. Polym. 2020; 69(2):251-255.
Alwossabi AM, Elamin ES, Ahmed EM, Abdelrahman M. Solubility enhancement of some poorly soluble drugs by solid dispersion using Ziziphus spina-christi gum polymer. Saudi Pharm J. 2022; 30(6):711-725.
Pardeshi SR, More MP, Patil PB, Mujumdar A, Naik JB. Statistical optimization of voriconazole nanoparticles loaded carboxymethyl chitosan-poloxamer based in situ gel for ocular delivery: In vitro, ex vivo, and toxicity assessment. Drug Deliv. Transl. 2022; 12(12):3063-3082.
Vasconcelos T, Marques S, das Neves J, Sarmento B. Amorphous solid dispersions: Rational selection of a manufacturing process. Adv. Drug Deliv. Rev. 2016; 100:85-101.
Kolimi P, Youssef AA, Narala S, Nyavanandi D, Dudhipala N, Bandari S, Repka MA. Development and characterization of itraconazole non-aqueous creams for the treatment of topical fungal infections. J. Drug Deliv. Sci. Technol. 2022;76:103818.
Kulkarni NS, Gite PD, Munde MK, Dhole SN, Khiste RH. A comprehensive review on application of microwave irradiation for preparation of inclusion complexes with cyclodextrins. Res J Pharm Technol. 2021; 14(2):1131-1136.
Chowhan A, Giri TK. Polysaccharide as renewable responsive biopolymer for in situ gel in the delivery of drug through ocular route. Int. J. Biol. Macromol. 150:559-572.
AboulFotouh K, Zhang Y, Maniruzzaman M, Williams III RO, Cui Z. Amorphous solid dispersion dry powder for pulmonary drug delivery: Advantages and challenges. Int. J. Pharm. 2020; 587:119711.
Irigoiti Y, Yamul DK, Navarro AS. Co-crystallized sucrose with propolis extract as a food ingredient: Powder characterization and antioxidant stability. LWT. 2021; 143:111164.
Nyavanandi D, Narala S, Mandati P, Alzahrani A, Kolimi P, Almotairy A, Repka MA. Twin Screw Melt Granulation: Alternative Approach for Improving Solubility and Permeability of a Non-steroidal Anti-inflammatory Drug Ibuprofen. AAPS PharmSciTech. 2023;24(1):47.
Basu B, Bagadiya A, Makwana S, Vipul V, Batt D, Dharamsi A. Formulation and evaluation of fast dissolving tablets of cinnarizine using superdisintegrant blends and subliming material. J. Adv. Pharm. Technol. Res. 2011; 2(4):266-272.
Yadav I, Rathnam VS, Yogalakshmi Y, Chakraborty S, Banerjee I, Anis A, Pal K. Synthesis and characterization of polyvinyl alcohol-carboxymethyl tamarind gum based composite films. Carbohydr. Polym. 2017; 165:159-68.
Chen YD, Liang ZY, Cen YY, Zhang H, Han MG, Tian YQ, Zhang J, Li SJ, Yang DS. Development of oral dispersible tablets containing prednisolone nanoparticles for the management of pediatric asthma. Drug Des Devel Ther. 2015; 9:5815.
Lavanya DK, Kulkarni PK, Dixit M, Raavi PK, Krishna LN. Sources of cellulose and their applications—A review. Int. J. Drug Dev. Res. 2011; 2(6):19-38.
Downloads
Published
Issue
Section
License
Copyright (c) 2024 Atish Velhal, Vijay Salunkhe
This work is licensed under a Creative Commons Attribution 4.0 International License.
