An Investigational Study For Screening Of Different Polymers For The Solubility Enhancement Of Pazopanib Hydrochloride Via Formulation Of Third-Generation Solid Dispersion.
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Abstract
In the conducted research study, solubility investigation was performed to elucidate the dissolution rate and behaviour of a drug incorporated within a solid dispersion matrix. The foremost objective was to appraise the impact of formulation parameters on the improvement of drug's solubility, the list of factors influencing the bioavailability. To this end, a systematic series of experiments were undertaken, wherein the drug was co-precipitated with a hydrophilic polymer carrier using various solvent systems and ratios. The resulting solid dispersions were meticulously characterized, employing state-of-the-art analytical techniques. Subsequently, solubility profiles were generated through equilibrium solubility studies, encompassing a range of pH conditions and temperatures, to comprehensively evaluate the dissolution behaviour of the drug. Based on study, it was concluded that the solubility of Pazopanib Hydrochloride (Pazopanib base) is significantly increased from 0.001 mg/ml to ~8.000 mg/ml. the same was confirmed from the analytical tools. Analytical tools also confirm the conversion of crystalline form to amorphous form. The outcomes of these investigations provide essential insights into the potential utility of solid dispersion systems as a viable strategy for enhancing the solubility and, consequently, the therapeutic efficacy of the drug in question.
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References
Baghel S, Cathcart H, O’Reilly NJ. Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs. J Pharm Sci [Internet]. 2016;105(9):2527–44. Available from: http://dx.doi.org/10.1016/j.xphs.2015.10.008
Deshmukh AS, Tiwari KJ, Mahajan VR. Solubility Enhancement Techniques for Poorly Water-Soluble Drugs Solubility Enhancement Techniques for Poorly Water-Soluble Drugs. 2018;(April 2017).
B. Maddiboyina, J. Shanmugapriya, S. Rasala, G. Sivaraman, In Bioinspired Nanomaterials: Synthesis and Emerging Applications, Materials Research Forum LLC, 2021;111:63–95.
Geel RMJM, Beijnen JH, Schellens JHM. Concise Drug Review: Pazopanib and Axitinib. Oncologist. 2012;17(8):1081–9.
Miyamoto S, Kakutani S, Sato Y, Hanashi A, Kinoshita Y, Ishikawa A. Drug review: Pazopanib. Jpn J Clin Oncol. 2018;48(6):503–13.
Verheijen RB, Beijnen JH, Schellens JHM, Huitema ADR, Steeghs N. Clinical Pharmacokinetics and Pharmacodynamics of Pazopanib: Towards Optimized Dosing. Clin Pharmacokinet. 2017;56(9):987–97.
Fda. PAZOPANIB: FDA Prescribing Information. 2009;1–18. Available from: papers2://publication/uuid/CBAA51C3-5418-4B85-BABB-7C92BB885302
Rendell J, Kwokal A. Process for the preparation of pazopanib hcl and crystalline forms of pazopanib hcl. 2010;1–19.
Ellakwa TE, Ellakwa DE. Enhancement of the solubility and the dissolution rate of oral nimodipine formulation with solid dispersion. Egypt J Chem. 2021;64(2):721–8.
H. Roy, B.S. Nayak, B. Maddiboyina, S. Nandi, Chitosan based urapidil microparticle development in approach to improve mechanical strength by cold hyperosmotic dextrose solution technique, J. Drug Deliv. Sci. Technol. 76 (2022) 103745.
Maddiboyina B, Roy H, Nakkala RK, Gandhi S, Kavisri M, Moovendhan M. Formulation, optimization and characterization of raloxifene hydrochloride loaded PLGA nanoparticles by using Taguchi design for breast cancer application. Chem Biol Drug Des. 2023 Sep;102(3):457-470.
Paradkar A, Ambike AA, Jadhav BK, Mahadik KR. Characterization of curcumin-PVP solid dispersion obtained by spray drying. Int J Pharm. 2004;271(1–2):281–6.
Quinn M. Pharmaceutical Analysis Using UV-Vis : Compliance with USP. :1–6.
Balaji M, Ramyakrishna N, Hanumanaik M. Formulation Development and Characterization of Enteric Coated Tablets of Lansoprazole. der Pharm Lett. 2020;12(3):22-38.
Kumar S, Parkash C, Kumar P, Singh SK. Application of Some Novel Techniques for Solubility Enhancement of Mefenamic Acid , A Poorly Water Soluble Drug. Int J Pharm Sci Drug Resesarch. 2009;1(3):164–71.
Sood S, Maddiboyina B, Rawat P, et al. Enhancing the solubility of nitazoxanide with solid dispersions technique: formulation, evaluation, and cytotoxicity study. J Biomater Sci Polym Ed. 2020;12(3):22-38.
Mamdouh MA, Badawi AA, Sakaran WS, Elshafeey AH, Elnahas OS. Different Solid Dispersion Techniques for Dissolution Enhancement Using Paracetamol as a Model Drug. Int J Pharm Phytopharm Res. 2015;4(2):231–7.
Yamashita K, Nakate T, Okimoto K, Ohike A, Tokunaga Y, Ibuki R, et al. Establishment of new preparation method for solid dispersion formulation of tacrolimus. Int J Pharm. 2003;267(1–2):79–91.
Maddiboyina B, Ramaiah, Nakkala RK, Roy H. Perspectives on cutting-edge nanoparticulate drug delivery technologies based on lipids and their applications. Chem Biol Drug Des. 2023 Aug;102(2):377-394.