FORMULATION AND CHARACTERIZATION OF MICROSPHERES OF NITAZOXANIDE BY CHEMICAL CROSSLINKING METHOD
The work investigated the design and evaluation of microspheres of Nitazoxanide by Ionotropic gelation technique met. 32 Factorial designs were used and concentration of polymer carbopol-934 (X1) and Ethyl cellulose (X2) were selected as the independent variables. The surface morphology study by SEM indicated that microspheres were spherical with smooth surface. There was no interaction between the drug and polymers, as studied by FTIR study. The prepared microspheres were characterized by entrapment efficiency, particle size micromeritic properties. It was observed that on increasing polymer concentration of formulations, % yield, the entrapment efficiency and particle size were increased whereas % drug release decreased. The In Vitro release study was done using U.S.P. dissolution rate basket type apparatus in phosphate buffer pH 7.4 for 10 hr. It shows that on increasing polymer concentration the drug release of all formulations was gradually decreased. In Vitro mucoadhesion study depicts that as the polymer concentration increased, mucoadhesive nature of the formulation was also increased. The microspheres of NTZ (formulation F9) showed best results due to highest drug entrapment efficiency (85.50%), and percentage drug release after 10.0 hr. was 50.25%. The rate of release followed First order kinetics. The microspheres exhibits good mucoadhesive properties in in- vitro wash-off test at pH 7.4 (Intestinal pH) than pH 1.2 (gastric pH),because the drug was completely absorbed in Gastrointestinal tract, Therefore, it can be concluded that Nitazoxanide Loaded algino-carbopol-934 microspheres can be formulated for sustained drug delivery of Nitazoxanide used in Chronic Hipatitis-C.
Keywords: Mucoadhesive microspheres, Nitazoxanide, Carbopol-934, Ethyl cellulose, Sodium Alginate, Factorial design.
2. Bhowmik D, Gopinath H, A Review on Control Release Drug Delivery System. The Pharma Innovation, 2012; 1:25-26.
3. Betram G, Katzung, Susane BM. Basic Clinical pharmacology. 11th ed. Tata Mc Graw Hill publication; 2010. P. 918.
4. Bhale S, Patankar RD, RP HPLC Development and validation of Nitazoxanid in Tablet dosage form, International Journal of Pharmacy and Pharmaceutical Sciences, 2011; 3(3):71-73.
5. Kappor D, Patel M, Vyas R, Lad C, Tyagi B. A review on microsponge drug delivery system. Journal of Drug Delivery and Therapeutics, 2014; 4(5):29-35. https://doi.org/10.22270/jddt.v4i5.978
6. Deshmukh VN, Jadhav JK, “Formulation, Optimization and Evaluation of Controlled Release Alginate Microspheres Using Synergy Gum Blends” Research J. Pharm. and Tech, 2009; 2:324-328.
7. Desh P, MM, Soni CS, UV Spectrophotometric estimation of NTZ in Tablet dosages form, Research journal of pharmacy and technology, 2011; 4:1714.
8. Dhakar RC, Maurya SD, Aggarawal S, Kumar G, Tilak VK, Design and evaluation of SRM Microspheres of Metformin Hydrochloride, International Journal of Comperhensive Pharmacy 2010; 1(1):1-5.
9. Deshmukh T, Deshmukh V, “Formulation and Evaluation of Mucoadhesive Microspheres of Ziprasidone Hydrochloride for Oral Controlled Release” Current Pharm Research, 2012; 2(2):497-502.
10. Dusane A, Rattilal, A Review on Sustained release technology, International journal of research in Ayurveda & pharmacy, 2011; 12:1708.
11. Garg A, Upadhyay P, Mucoadhesive microspheres review, Asian Journal of Pharmaceutical and Clinical Research, 2012; 5:24-27.
12. Hardenia SS, Jain A, “Formulation and Evaluation of Mucoadhesive Microspheres of Ciprofloxacin, Journal of Advanced Pharmacy Education & Research, 2011; 1(4):214-224.
13. Jadhav V, Gandhi SV, RP-HPLC Determination of Nitazoxanide in Bulk and Different Tablet Formulations, Eurasian Journal of Analytical Chemistry, 2008; 3:318-323.
14. Jenifer LH, A Review: Current approaches to treatment of gastrointestinal infection Focus NTZ, 2009, 263-275.
15. Khan S, Tiwari T, A Review On Microspheres. World Journal of Pharmacy and Pharmaceutical Sciences, 2012; 1:126-130.
16. Kataria S,Middha A, A Review On Microsphere. International Journal of Research in Pharmacy & Chemistry, 2011; 1:1186-1193.
17. Kumar S, Singh J, Design and Characterization of Amoxicillin trihydrate Mucoadhesive Microspheres for Prolonged Gastric retention, International Journal of Pharmaceutical Sciences and Drug Research, 2010; 2(2):112-114.
18. Keerthi TS, Kumar S, “Formulation and evaluation of microspheres of Losartan Potassium using biodegradable natural polymers” International Bulletin of Drug Research, 2012; 1(2):120-131.
19. Kapoor D, Patel R, “Formulation, Optimization and Evaluation of Floating Microspheres of Captopril” Asian Journal of biomedical &Pharmaceutical Sciences, 2012; 2(9):1-10.
20. Rastogi V, Shukla S, Singh R, Lal N, Yadav P. Microspheres: a promising drug carrier. Journal of Drug Delivery and Therapeutics, 2016; 6(3):18-26. https://doi.org/10.22270/jddt.v6i3.1196
21. Kumar S, Senthil S, Kumar A, Evaluation of Clobazam loaded ionically cross-linked microspheres using Chitosan, Available online at www.pelagiaresearchlibrary.com, 2012; 3(6):616-623.
22. Kumar S, Kumar A, “Formulation and Evaluation of Colon Targeted Drug Delivery of an Anti-Amoebic Drug” International Journal of Pharmaceutical Innovations, 2012; 2(2):138-143.
23. Lachman L, Lieberman HA, Kanig JL. The theory and practice of industrial pharmacy. 3rd ed. Mumbai: Verghese Publishing House; 1991. P. 254 -255.
24. Josephine J, Mehul RT, “Formulation and In Vitro Evaluation of Floating Microspheres of Anti-Retro Viral Drug as a Gastro retentive Dosage” International Journal of Research in Pharmacy Chemistry, 2011; 1(3):2231-2781.
25. Ahmed MG, Dr. Nagesh, Design of minocycline Hydrochloride Microspheres Loacal delivery in Treatment of Periodontitis, International Journal of Advance Pharmaceutical and Biological Sciences, 2012; 2(4):245-249.
26. Faizi M, Venkatesh MN, “Formulation and Evaluation of Mucoadhesive Microspheres of Amoxicillin Trihydrate by using Eudragit RS 100” International Journal of Chem Tech Research, 2010; 2:466-470.
27. Agarwal D, Ranawat M, Chauhan C, Kamble R. Formulation and charecterisation of colon targeted ph dependent microspheres of capecitabine for colorectal cancer. Journal of Drug Delivery and Therapeutics, 2014; 3(6):215-222. https://doi.org/10.22270/jddt.v3i6.747
28. Mehta D, Seth AK, “HPLC Method for Simultaneous estimation of Nitazoxanide in its Tablet dosage form” An International Journal of pharmaceutical Sciences, 2011; 2(4):1-12
29. Khanam N, Sachan AK, Fabrication and evaluation of Propranolol hudrochloride loaded microspheres by Ionic-gelation technique, At www.scholers research library, 2012; 4:815-820.
30. Ali NW, Abbas SS, Validation Stability indicating methods for determination of Nitazoxanide in presence of its degradation products, Journal of pharmaceutical analysis, 2012; 2:105-116.
31. Pavanveena, Chintagunta, Kavitha K, “Formulation and evaluation of Trimetazidine Hydrochloride loaded chitosan microspheres” International Journal of Applied Pharmaceutics, 2010; 2(2):11-15.
32. Parashar V, Ahmad D, “Formulation and evaluation of biodegradable microspheres of tinidazole” International Journal of Drug Deliver, 2010; 2:238-241.
33. Senthil PS, Sandu NR, Loganathan S, Formulation and evaluation of Microspheres Containing Imatinib Mesylate using Sodium Alginate By Chemical Crosslinking Method, Journal of Drug Delivery and Therapeutics, 2012; 2(6):37-40. https://doi.org/10.22270/jddt.v2i6.339
34. Pundir S, Badola A, A Review on Sustained Release matrix Tech. & Recent Advances in matrix drug delivery system, Inter. Jour. of Res. and Tech, 2013; 3:12-13.
35. Patel B, Modi V, Preparation and evaluation of ethyl Cellulose Microspheres Prepared by emulsification-Solvent evaporation method, International Journal for Research in Management and Pharmacy (IJRMP), 2012; 1(1):82-92.
36. Patel RJ, Singh BH, RP HPLC Method for estimation of nitazoxanide in oral suspension formulation, Der Pharma Chemica, 2012; 4(3):1140-1144.
37. Venkatesh PD, Karki R, “Formulation and Evaluation of Microspheres Containing Fluvastatin Sodium” International Journal of Drug Development & Research, 2012; 4(2).
38. Gupta M, Khunteta A. Optimization of the release kinetics of diltiazem hydrochloride from tableted microspheres. Journal of Drug Delivery and Therapeutics, 2018; 8(1):57-63. https://doi.org/10.22270/jddt.v8i1.1551
39. Rajput S, Agrawal P, A Review on microspheres: methods of preparations and evaluation, World Journal 0f Pharmacy and Pharmaceutical Sciences, 2012; 1:422-438.
40. Rowe CR, Sheskey P. A Hand Book of Pharmaceutical Excipients, 6th ed. Php Pharmaceutical Press; 2010. P .450-858.
41. Massa-Reddy RS, Bolmad VB, Metformin HCl loaded Sod.Alginate Floating Microspheres, Indian Journal of Novel Drug Delivery, 2011, 126-143.
42. Reddy VV, Swaroop AP, Preparation and In-Vitro Evaluation of Lansoprzole mucoadhessive microspheres, An International Journal of Advances in Pharmaceutical Sciences, 2011, 2.
43. Sharifa S, Ahammad T, RP-HPLC Method development and Validation for Nitazoxanide in Powder for suspension dosage form, International Journal of Pharmaceutical Science and Research, 2013; 4(1):301-305.
44. Dehghan S, Aboofazeli R, “Formulation optimization of Nifedipine containing microspheres using factorial design” Affrican journal of pharmacy and pharmacology, 2010; 4:346-354.
45. Murathoti K.S., Saxena T. Development of mucoadhesive microspheres of levofloxacin for the treatment of H. pylori infection. Journal of Drug Delivery and Therapeutics, 2016; 6(1):34-45. https://doi.org/10.22270/jddt.v6i1.1179
46. Singh A, Sharma R, A Review Article on Sustained release drug delivery system, Int. Res. Journal of Pharmacy, 2012, 3, 22-23.
47. Steve, Bhaskara RD. Standard Hand Book of Biomedical Engineering & Design. 3rd ed. P. 223-224.
48. Senthil A, Thakkar HR, “Formulation and Evaluation of Mucoadhessive Glipizide Microspheres using Carboxy methyl Cellulose” International Journal of Preclinical and Pharmaceutical Research, 2011; 2(1):45-51.
49. Vyas SP, Khar RK. Targated and Control drug delivery. 4th ed. C.B.S. Publications; 2008. P. 418-454.
50. Steve-1, Bhaskara R. A Standard Hand Book of Biomedical engineering. P. 223-224.
51. Sagostarch SA, Journal of Biosciences and Bioengineering, 2002; 94(6):526-529.
52. Kumar TU, Kumar N, Design and evaluation of aceclofenac microspheres by solvent Evaporation technique, International Journal of Pharmaceutical Sciences Letters, 2013; 3(1):170-172.
53. Jilakara VS, Design and characterization of mucoadhesive microspheres loaded with Metronidazole for colon specific delivery, Current pharma research, 2013; 3:901-910.
54. Prasanth VV, Rawat S, “Formulation and Evaluation of Floating Microspheres of Captopril” International Journal of Research Article Pharmaceutical Innovations, 2013; 3(2):41-52.
55. Wadke DA,Serajuddin A, Jacobson H, Preformulation testing. In: Lieberman HA, Lachman L, Schwartz JB, eds. Pharmaceutical Dosage Forms: Tablets. New York: Marcel Dekker: 1989, 1-73.
56. Yadav A, Kumar JD, “Formulation and evaluation of mucoadhesive microspheres of propranolol hydrochloride for sustained drug delivery” Asian Journal of Pharmacy and Medical Science, 2011; 1 (1):1-8.
57. Zhang Y, Wei W, Preparation and evaluation of Alginate–chitosan microspheres for oral delivery of insulin, European Journal of Pharmaceutics and Biopharmaceutics, 2011; 77:11-19.
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported License. that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (SeeÂ The Effect of Open Access).