Author(s):
Saijyosthana Gandey, Vema Aparna, Raghupathi Kandarapu
Email(s):
jyothsnagandey@gmail.com
DOI:
10.5958/0974-360X.2020.00487.4 
Address:
Saijyosthana Gandey1*, Vema Aparna2, Raghupathi Kandarapu3
1MNR College of Pharmacy, Fasalwadi, Sangareddy, Telangana, India.
2College of Pharmacy, Konerulakshmaiah Education Foundation, Vaddeswaram, Guntur, India.
3Delexcel Pharma Private Limited, Manoharabad Mandal, Medak, Telangana, India.
*Corresponding Author
Published In:
Volume - 13,
Issue - 6,
Year - 2020
ABSTRACT:
The objective of present research was to formulate, optimize and characterize silybin microspheres using emulsion solvent evaporation method using a polymer, poly-e-caprolactone and an emulsifier, poly vinyl alcohol for sustained drug delivery. The microspheres were formulated using emulsion solvent evaporation method. The microspheres were optimized by taking different drug and polymer ratio (1:1 to1:8), emulsifier concentration (1%, 1.5%, 2% and 2.5%) and stirring speed (1000rpm, 1500rpm, 2000rpm, 2500rpm, 3000rpm). Then the microspheres were characterized for particle size, percentage yield, entrapment efficiency, scanning electron microscopy and in vitro drug release. The microspheres prepared by this method showed good entrapment efficiency and percentage yield. From the Fourier Transform Infrared Spectroscopic studies it was revealed that there were no significant interactions between silybin and excipients. Scanning Electron Microscopic photographs revealed that the microspheres were in spherical shape and smooth. Drug release studies revealed good release following korsmeyer peppas model indicating drug Non fickian diffusion mechanism. It was clearly observed that increase in polymer content, increased the dug entrapment up to a certain level, and then decreased. The other process variables like stirring speed and concentration of emulsifier also influenced the entrapment efficiency and drug release. In conclusion, Silybin was conveniently formulated as polymeric microspheres by emulsion solvent evaporation method. Formulation with 1:4 drug polymer ratio, 2% emulsifier with 2000 rpm was selected as optimized formulation.
Cite this article:
Saijyosthana Gandey, Vema Aparna, Raghupathi Kandarapu. Preparation and Optimization of Silybin sustained release Microspheres for the treatment of Liver Disorders. Research J. Pharm. and Tech 2020; 13(6): 2742-2748. doi: 10.5958/0974-360X.2020.00487.4
Cite(Electronic):
Saijyosthana Gandey, Vema Aparna, Raghupathi Kandarapu. Preparation and Optimization of Silybin sustained release Microspheres for the treatment of Liver Disorders. Research J. Pharm. and Tech 2020; 13(6): 2742-2748. doi: 10.5958/0974-360X.2020.00487.4 Available on: https://rjptonline.org/AbstractView.aspx?PID=2020-13-6-37
REFERENCES:
1. Vladimir Krena, Daniela Walterova. Silybin and silymarin– New effects and applications. Biomed. Pap 2005; 149(1):29–41.
2. J. H. Tsai, J. Y. Liu, T. T. Wu, P. C. Ho, C. Y. Huang, J. C. Shyu, Y. S. Hsieh, C. C. Tsai et al. Effects of silymarin on the resolution of liver fibrosis induced by carbon tetrachloride in rats. J. Viral Hepatitis 2008; 15:508–514.
3. Loguercio C, Festi D. Silybin and the liver: From basic research to clinical practice. World J Gastroenterol 2011; 17(18): 2288-301.
4. Petra Janc ova, Eva Anzenbacherova, Barbora Papouskova, Karel Lemr, PavlaLuz na, Alena Veinlichova et al. Silybin Is Metabolized by Cytochrome P450 2C8 in vitro. Drug Metab. Dispos 2007; 35: 2035–39.
5. Somya Gupta, Nayyar Parvez, Akanksha Bhandari, Pramod K. Sharma. Microspheres based on herbal actives: the less-explored ways of disease treatment. Egypt. Pharm. J 2015; 14:148–157.
6. Rameshwar K. Deshmukh, Jitendra B. Naik.Diclofenac Sodium-Loaded Eudragit Microspheres: Optimization Using Statistical Experimental Design. J. Pharm. Sci. Innovation 2013; 8(4):276-287.
7. M.D.AbEl-Hameed, I.W.Kellaway. Preparation and in vitro characterisation of mucoadhesive polymeric microspheres as intra-nasal delivery systems. Eur. J. Pharm. Biopharm 1997; 44(1): 53-60.
8. Rathor Shruti, Ram Alpana. Formulation and Characterization of Biocompatible Microspheres of Benzophenone-3. Research J. Pharma. Dosage Forms and Tech. 2009; 1(3):222-225.
9. Vinod R, Ashok Kumar P, Amit S Yadav, Someshwara Rao B, Suresh V Kulkarni. Formulation and Evaluation of Controlled Release Microspheres of Zidovudine. Research J. Pharma. Dosage Forms and Tech. 2010; 2(1):96-99.
10. Rajesh H. Parikh, Jolly R. Parikh, Rajesh R. Dubey, Heena N. Soni, Kishor N. Kapadia. Poly (D, L-Lactide-Co-Glycolide) microspheres containing 5-fluorouracil: Optimization of process parameters. AAPS PharmSciTech 2003; 4(2): 14-28.
11. Iosif Daniel Rosca, Fumio Watarib, MotohiroUo. Microparticle formation and its mechanism in single and double emulsion solvent evaporation. J. Controlled Release 2004; 99: 271–280.
12. Devesh Kapoor, Rakesh Patel. Formulation, Optimization and Evaluation of Floating Microspheres of Captopril. Asian J. Biomed. Pharm. Sci 2012; 2(9): 1-10.
13. Amitava Ghosh, Udaya Kumar Nayak, Prasant Rout, Tanusree Nag, Partha Roy. Preparation, Evaluation and in vitro- in vivo Correlation (IVIVC) study of Lamivudine Loaded Microspheres. Research J. Pharm. and Tech. 1(4): Oct.-Dec. 2008: 353-356.
14. Kalla Madhavi, S Shobha Rani, Shaheda Khatoon, ChoppariVijender. Preparation, Optimization and Characterization of Eudragit Coated Chitosan Piroxicam Microspheres Intended for the Treatment of Rheumatoid Arthritis. Pharm Anal Acta 2016; 7: 485-492.
15. He Zhang, Ying Lu, Guoqing Zhang, Shen Gao, Duxin Sun, Yanqiang Zhong. Bupivacaine-loaded biodegradable poly (lactic-co-glycolic) acid microspheres: I. Optimization of the drug incorporation into the polymer matrix and modelling of drug release. Int. J. Pharm 2008; 351(1-2): 244-249.
16. Manish P Patel, MM Patel, KN Patel, DR Patel, UL Patel. Designing and Evaluation of Floating Microspheres of Verapamil Hydrochloride: Effect of Methocel. Research J. Pharma. Dosage Forms and Tech. 2009; 1(1): 22-28.
17. Kumar Darapu B.N., K. Sundaramoorthy, T.Vetrichelvan. Formulation and In-Vitro Evaluation of Gastroretentive Floating Microspheres of Ranitidine Hydrochloride. Research J. Pharma. Dosage Forms and Tech. 2011; 3(1): 24-29.
18. Singh Bandana, KanoujiaJovita, Pandey Manisha, SarafShubhini A. Formulation and Evaluation of Floating Microspheres of Famotidine. Int. J. PharmTech Res 2010; 2(2): 1415-20.
19. Harshad Parmar, Sunil Bakliwal, Nayan Gujarathi, Bhushan Rane, Sunil Pawar. Different methods of formulation and evaluation of mucoadhesive microspheres. Int. J. Appl. Biol. Pharm. Technol 2010; 1(3):1157-67.
20. S. Ramya Sri. Formulation and Evaluation of Nizatidine Microspheres. Research J. Science and Tech. 2019; 11(1):14-26.
21. Swati S Talokar, Rohan R Vakhariya. Formulation and Evaluation of Lomefloxacin Microspheres. Res. J. Pharm. Dosage Form. and Tech. 9(1): Jan.-Mar. 2017: 01-05.
22. Praveen Kumar Gaur, Shikha Mishra, Meenakshi Bajpai. Formulation and evaluation of controlled-release of telmisartan microspheres: In vitro/in vivo study. J. Food Drug Anal 2014; 22(4): 542-548.
23. Jong-Cheol Jeong, Jaeyoung Lee, Kilwon Cho. Effects of crystalline microstructure on drug release behavior of poly(q-caprolactone) microspheres. J. Controlled Release 2003; 92:249 – 58.
24. Varma Kumar Ajit, Gupta Kumar Arun, Khare Piush, Patel Rakesh. Formulation and Development of Floating Microspheres containing Levodopa and Carbidopa. Asian J. Pharm. Tech. 2018; 8 (4):200-202.
25. Phalguna Yadagiri, Rama Rao Korapati. Formulation, Characterization and In Vitro Evaluation of Lamivudine Microspheres. Asian J. Res. Pharm. Sci. 2016; 6(4): 235-239.
26. A Saravanakumar, Sunita Minz, Madhulika Pradhan, Pavani Sure, Atul N Chandu, Umesh Mishra, K Kamalakannan, T Sivakumar. Polylactic Acid Microspheres as A Potential Vaccine Delivery System for the Tetanus Toxoid: Preparation and In Vitro Dissolution Study. Research J. Pharm. and Tech. 1(4): Oct.-Dec. 2008:453-459.
27. Bohrey, S., Chourasiya, V. and Pandey, A. Polymeric nanoparticles containing diazepam: preparation, optimization, characterization, in-vitro drug release and release kinetic study. Nano Convergence, 2016; 3 (3) 0061-66
28. Yang, Y.Y.; Chung, T.S.; Ng, N.P. Morphology, drug distribution, and in vitro release profiles of biodegradable polymeric microspheres containing protein fabricated by double-emulsion solvent extraction/evaporation method. Biomaterials 2001; 22, 231–241.
29. Moussa, Dima and Kassab, Rima and Yammine, Paolo. Study of Diferent Processing parameters for Polylactic acid Microspheres Formulations. IJPSR 2014; 5(10): 4176-81.
30. Utsav C. Rathod, Anandk kumar K. Patel, Dushyant A. Shah. Statistical Evaluation and Optimization of Influence of Stirring Speed and Polymer Concentration on Hollow Microspheres of Diltiazem HCl. Der Pharmacia Lettre, 2012, 4 (3):972-978.