PREPARATION AND EVALUATION OF TMC LOADED VORICONAZOLE NANOPARTICLES
Keywords:Voriconazole, Tri-methyl chitosan, Nanoparticles, Opthalmic drug delivery system
Objective: Ocular diseases affect a growing number of people across the globe. Hence, the present research work focused to prepare and evaluate voriconazole (VCZ) nanoparticles containing trimethyl chitosan (TMC) for ophthalmic drug delivery with primary goal is to develop topical ocular delivery systems with improved ocular bioavailability and reduced systemic side effects while maintaining the dosage form’s simplicity and convenience.
Methods: In the present study, the nanoparticles are prepared using ionotropic gelation method. The physiochemical interactions between drugs and selected excipients were studied using various techniques such as FTIR, DSC, XRD, and H-NMR. The physiochemical properties of the nanoparticles such as size, PDI, pH, and drug content/entrapment efficiency were determined. The in-vitro drug release properties were characteristics and examined for the formulations. The synthesize form of chitosan, that is, tri-methyl chitosan is used due to solubility issue.
Result: The comparative study was done using TMC and cyclodextrin as a polymer out of which TMC polymer gives better results. The optimization is done using 32 factorial design using design expert software. The optimized batch follows the zero order release kinetics.
Conclusion: TMC loaded VCZ nanoparticles show better result with improved solubility and permeability.
Asasutjarit R, Theerachayanan T, Kewsuwan P, Veeranodha S, Fuongfuchat A, Ritthidej GC. Development and evaluation of diclofenac sodium loaded-N-trimethyl chitosan nanoparticles for ophthalmic use. AAPS PharmSciTech 2015;16:1013-24. doi: 10.1208/ s12249-015-0290-4, PMID 25609376
Bunjes H, Unruh T. Characterization of lipid nanoparticles by differential scanning calorimetry, X-ray and neutron scattering. Adv Drug Deliv Rev 2007;59:379-402. doi: 10.1016/j.addr.2007.04.013, PMID 17658653
Donohue EK, Wilensky JT. Dorzolamide: A review. In: Seminars in Ophthalmology. Vol. 12. United Kingdom: Taylor and Francis; 1997. p. 119-26.
Felt O, Furrer P, Mayer JM, Plazonnet B, Buri P, Gurny RJ. Topical use of chitosan in ophthalmology: Tolerance assessment and evaluation of precorneal retention. Int J Pharm 1999;180:185-93. doi: 10.1016/ s0378-5173(99)00003-4, PMID 10370189
Fouda NH, Abdelrehim RT, Hegazy DA, Habib BA. Sustained ocular delivery of dorzolamide-HCl via proniosomal gel formulation: In-vitro characterization, statistical optimization, and in-vivo pharmacodynamic evaluation in rabbits. Drug Deliv 2018;25:1340-9. doi: 10.1080/10717544.2018.1477861, PMID 29869516
Gupta KC, Ravi Kumar MN. An overview on chitin and chitosan applications with an emphasis on controlled drug release formulations. J Macromol Sci C 2000;40:273-308. doi: 10.1081/ MC-100102399
Harikumar SL, Sonia A. Nanotechnological approaches in ophthalmic delivery systems. Int J Drug Dev Res 2011;3:9-19.
Kashin AS, Ananikov VP. A SEM study of nanosized metal films and metal nanoparticles obtained by magnetron sputtering. Russ Chem Bull 2011;60:2602-7. doi: 10.1007/s11172-011-0399-x
Kesarla R, Tank T, Vora PA, Shah T, Parmar S, Omri A. Preparation and evaluation of nanoparticles loaded ophthalmic in situ gel. Drug Deliv 2016;23:2363-70. doi: 10.3109/10717544.2014.987333, PMID 25579467
Li J, Jin X, Yang Y, Zhang L, Liu R, Li Z. Trimethyl chitosan nanoparticles for ocular baicalein delivery: Preparation, optimization, in vitro evaluation, in vivo pharmacokinetic study and molecular dynamics simulation. Int J Biol Macromol 2020;156:749-61. doi: 10.1016/j.ijbiomac.2020.04.115, PMID 32320806
Malik A, Gupta M, Mani R, Gogoi H, Bhatnagar R. Trimethyl chitosan nanoparticles encapsulated protective antigen protects the mice against anthrax. Front Immunol 2018;9:562. doi: 10.3389/fimmu.2018.00562, PMID 29616046
Marangon FB, Miller D, Giaconi JA, Alfonso EC. In vitro investigation of voriconazole susceptibility for keratitis and endophthalmitis fungal pathogens. Am J Ophthalmol 2004;137:820-5. doi: 10.1016/j.ajo.2003.11.078, PMID 15126145
Min JB, Kim ES, Lee JS, Lee HG. Preparation, characterization, and cellular uptake of resveratrol-loaded trimethyl chitosan nanoparticles. Food Sci Biotechnol 2018;27:441-50. doi: 10.1007/s10068-017-0272- 2, PMID 30263768
Mourya VK, Inamdar NN. Chitosan-modifications and applications: Opportunities galore. React Funct Polym 2008;68:1013-51. doi: 10.1016/j.reactfunctpolym.2008.03.002
Munier A, Gunning T, Kenny D, O’Keefe M. Causes of blindness in the adult population of the republic of Ireland. Br J Ophthalmol 1998;82:630-3. doi: 10.1136/bjo.82.6.630, PMID 9797662
Naik JB, Pardeshi SR, Patil RP, Patil PB, Mujumdar A. Mucoadhesive micro-/Nano carriers in ophthalmic drug delivery: An overview. BioNanoScience 2020;10:564-82. doi: 10.1007/s12668-020-00752-y
Üstündağ Okur NÜ, Yozgatlı V, Okur ME, Yoltaş A, Siafaka PI. Improving therapeutic efficacy of voriconazole against fungal keratitis: Thermo-sensitive in situ gels as ophthalmic drug carriers. J Drug DelivSci Technol 2019;49:323-33. doi: 10.1016/j.jddst.2018.12.005
Pandit J, Sultana Y, Aqil M. Chitosan-coated PLGA nanoparticles of bevacizumab as novel drug delivery to target retina: Optimization, characterization, and in vitro toxicity evaluation. Artif Cells Nanomed Biotechnol 2017;45:1397-407. doi: 10.1080/21691401.2016.1243545, PMID 27855494
Shastri D, Shelat P, Shukla A, Patel P. Ophthalmic drug delivery system: Challenges and approaches. Syst Rev Pharm 2010;1:113-20. doi: 10.4103/0975-8453.75042
Popa L, Ghica MV, Dinu-Pîrvu CE, Irimia T. Chitosan: A good candidate for sustained release ocular drug delivery systems. In: Chitin- Chitosan-Myriad Functionalities in Science and Technology. London, UK: InTech; 2018. p. 283-310.
Shinde UA, Joshi PN, Jain DD, Singh K. Preparation and evaluation of N-trimethyl chitosan nanoparticles of flurbiprofen for ocular delivery. Curr Eye Res 2019;44:575-82. doi: 10.1080/02713683.2019.1567793, PMID 30632402
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