DESIGN, 23 FACTORIAL OPTIMIZATION AND IN VITRO – IN VIVO PHARMACOKINETIC EVALUATION OF ROSUVASTATIN CALCIUM LOADED POLYMERIC NANOPARTICLES
Keywords:Rosuvastatin Calcium, Polymeric nanoparticle, Bioavailability, Pharmacokinetic, Zetapotential
Objective: The objective is to incorporate low bioavailable Rosuvastatin Calcium (20%) into polymeric nanoparticles (PNs) to improve its biopharmaceutical properties of Rosuvastatin Calcium.
Methods: The PNs were prepared by solvent evaporation method by applying 23 factorial designs. The formulated PN are investigated for particle size (PS) and shape, zeta potential (ZP), polydispersity index (PI) and entrapment efficiency (EE), in-vivo pharmacokinetic.
Results: Among 8 formulations, PN7 shows least PS of 159.9±16.1 nm which enhance the dissolution, surface area and permeability; ZP of -33.5±1.54 mV which shows good stability; PI of 0.587±0.16 shows monodisperse distribution pattern; high EE of about 94.20±2.46 %; percentage yield of 96.80±2.08 %; maximum in-vitro drug release of about 96.54±2.02 % at 24 h with controlled and predetermined release pattern. PN7 drug release obeys zero order release kinetics, non-fickian diffusion mechanism with r2 value > 0.96 and release exponent ‘n’ value falls between 0.5-0.8 for peppas kinetic model i.e., the mechanism of drug diffusion is based on polymer relaxation. In vivo pharmacokinetic studies illustrate enhance in AUCo-α in mg/ml, which proves a significant enhancement of bioavailability of Rosuvastatin Calcium by PNs.
Conclusion: This PN shows a significant enhancement of bioavailability by minimizing the dose-dependent adverse side effects of Rosuvastatin Calcium.
Carina IC Crucho, Maria Teresa Barros. Polymeric nanoparticles: A study on the preparation variables and characterization methods. Mater Sci Eng C 2017; 80: 771-84.
Khalid M El-Say, Hossam S El-Sawy. Polymeric nanoparticles: Promising platform for drug delivery. Int J Pharm 2017; 528: 675-91.
El-Say KM, El-Sawy HS. Polymeric nanoparticles: Promising platform for drug delivery. Int J Pharm. 2017; 528:675-91.
Yadhav KS, Nagavarma BVN, Hemant. Different techniques for preparation of polymeric nanoparticles. Asian J Pharm Clin Res 2012; 5: 16-23.
Aleksandra Zieli nska, Filipa Carreiro, Ana M. Oliveira. Polymeric Nanoparticles: Production, Characterization, Toxicology and Ecotoxicology. Molecules 2020; 25: 1-20.
Savita Bisht. Polymeric nanoparticles-encapsulated curcumin (nanocurcumin): a novel strategy for human cancer therapy. J Nanobiotechnology 2007; 5: 1-18.
Namita Rajput. Method of preparation of nanoparticles. IJAET 2015; 7: 1806-11.
Dourado, D. Pharmaceutical Nanotechnology: A Therapeutic Revolution. Int J Pharm Sci Dev Res 2020; 6: 09–11.
Sovan Lal Pal. Nanoparticles: An overview of preparation and characterization. J Appl Pharm Sci 2011; 1: 228-34.
Jonghwi Lee, Hesson Chung. Methods of preparation of drug nanoparticles. Wiley online library. 2007:14-19.
Iravani S. Synthesis of nanoparticles: Physical, chemical & biological methods. Res Pharm Sci 2014; 5: 113-20.
Owens, Peppas A. Opsonisation, Biodistribution, and pharmacokinetics of polymeric nanoparticles. Int J Pharm 2006; 307:93-102.
Krishna Gudikandula. Synthesis of silver nanoparticles by chemical and biological methods and their antimicrobial properties. J Exp Nanosci 2016; 11:714-21.
Helmut Schmidt. Nanoparticles by chemical synthesis, processing to materials & innovative applications. Appl Organomet Chem 2001; 15:331-43.
Zhipeng Gu, Jun Wu. Polymeric nanoparticles for colon cancer therapy: overview and perspectives. J Mater Chem B. 2016; 48:7779-92.
Norouzi Banis H. Synthesis of silicide nanomaterials using chemical vapour deposition method. E theses and dissertations 2012; 767: 50-66.
Xia W, Alexander Birkner. Chemical vapour deposition and synthesis on carbon nanofibres. Chem Mater 2005; 17(23):5737-42.
Karthik S, Avijit Jana Coumarin polycarprolactone polymeric nanoparticles. J Mater Chem B 2017; 5:1734-41.
Nancy M Elbaz. Core-Shell Silver polymeric nanoparticles-based combinational therapy against Breast cancer In Vitro. Sci Rep 2016; 6: 1-9.
Shibata A. Polymeric nanoparticles containing combination of Antiretrovial Drugs. AIDS Res Hum Retroviruses 2013; 29:746-54.
Suphiya Parveen, Sanjeeb. Polymeric nanoparticles for cancer therapy. J Drug Target 2008; 16:108-23.
Khalid M. Polymeric nanoparticles: Promising platform for drug delivery. Int J Pharm 2017; 7: 675-91.
Gajra B, Patel RR, Dalwadi C. Formulation, optimization and characterization of cationic polymeric nanoparticles of mast cell stabilizing agent using the Box-Behnken experimental design. Drug Dev Ind Pharm. 2016; 42:747-57.
Amir Dustgania, Ebrahim Vasheghani Farahania, Mohammad Imanib. Preparation of Chitosan Nanoparticles Loaded by Dexamethasone Sodium Phosphate. Iranian J Pharma Sci 2008; 4: 111-4.
Zhang Z, Lee S H, Gan C W, Feng S S. Invitro and invivo investigation on PLA–TPGS nanoparticles for controlled and sustained small molecule chemotherapy. Pharm Res 2008; 25:1925–35.
Gabr MM, Mortada SM, Sallam MA. Hexagonal liquid crystalline nanodispersions proven superiority for enhanced oral delivery of Rosuvastatin Calcium: in vitro characterization and in vivo pharmacokinetic study. J Pharm Sci 2017; 106:3103–12.
Cooper KJ, Martin PD, Dane AL, Warwick MJ, Schneck DW, Cantarini MV. Effect of itraconazole on the pharmacokinetics of rosuvastatin. Clin Pharmacol Ther 2003; 73:322-9.
Kanukula R, Salam A, Rodgers A, Kamel B. Pharmacokinetics of Rosuvastatin: A Systematic Review of Randomised Controlled Trials in Healthy Adults. Clin Pharmacokinet. 2021;60:165-75.
E.BSoutoabS.AWissingaC.MBarbosabR.HMüller. Evaluation of the physical stability of SLN and NLC before and after incorporation into hydrogel formulations. Eur J Pharm Biopharm 2004; 58: 83-90.
Makoni PA, Wa Kasongo K, Walker RB. Short Term Stability Testing of Efavirenz-Loaded Solid Lipid Nanoparticle (SLN) and Nanostructured Lipid Carrier (NLC) Dispersions. Pharmaceutics. 2019; 11(8):397.
How to Cite
Copyright (c) 2021 SIVA PARAMESWARAN, GUDANAGARAM RAMAMOORTHY VIJAYASHANKAR, BENDI SRI VENKATESWARLU, RAJAPPA MARGRET CHANDIRA
This work is licensed under a Creative Commons Attribution 4.0 International License.