Asian Journal of Pharmacy and Technology

Open Access Open Access  Restricted Access Subscription Access
Open Access Open Access Open Access  Restricted Access Restricted Access Subscription Access

Formulation and Evaluation of Sustained Release Stavudine Microspheres by Ionotropic Gelation Method


Affiliations
1 Department of Pharmaceutics, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh, India
2 Department of Pharmaceutical Analysis, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh, India
3 Department of Chemistry, Vijaya Teja Degree College, Addanki - 523201, Andhra Pradesh, India
     

   Subscribe/Renew Journal


As a novel drug delivery system, microspheres improve the efficacy of a drug, increase the time of action, lower the number of times in which a dosage form needs to be administered, and to increase patient compliance. Oral administration side effects such as gastric irritation are lessened through the use of microspheres. Ionotropic gelation was used to create HPMC K15M, Guar gum, and Carbopol 934 microspheres with different concentrations of Carbopol 934 polymer. Cross-linking was accomplished with the use of calcium chloride. In order to conduct a systematic evaluation of all the preparations, we performed various tests: morphology, FTIR, DSC, entrapment efficiency, size, microsphere size, and in-vitro drug release. The discrete, free-flowing, and spherical particles of prepared Stavudine microspheres were found. In compliance with standards, the mean particle size was in the range of 72.64 to 95.22 percent. In vitro drug release studies were performed in phosphate buffer solution with a pH of 6.8. As the concentration of sodium alginate and calcium chloride increased, the percentage of drug release was reduced. In the case of F9 formulation, which contained Stavudine, the decreased drug release rate was obtained via carbopol 934(1:3), sodium alginate, and calcium chloride. Conclusively, the present study shows that Stavudine microsphere preparation and formulation F9 are successful. Stavudine microspheres must be prepared in order to preserve an effective drug concentration in serum for a long time, while reducing gastrointestinal irritation.

Keywords

Microspheres, Controlled Release, Stavudine, In-vitro Studies
Subscription Login to verify subscription
User
Notifications
Font Size


  • Nikam V, Gudoorkar V, Microspheres- A novel drug delivery system:an overview. Int J Pharma Chem Sci. 2012; 1(1):113-128.

  • Kristmundsdottir T, Ingvarsdottir K. Ibuprofen microcapsules: the effect of production variables on microcapsule properties. Drug Development and Industrial Pharmacy. 1994;20(5):769–778.

  • Capan Y, Jiang G, Giovagnoli S, Na K-H, DeLuca PP. Preparation and characterization of poly(D,L-lactide-co-glycolide) microspheres for controlled release of human growth hormone. AAPS PharmSciTech. 2003;4(2)

  • Gohel MC, Amin AF. Formulation optimization of controlled release diclofenac sodium microspheres using factorial design. Journal of Controlled Release. 1998;51(2-3):115–122.

  • Woo BH, Jiang G, Jo YW, DeLuca PP. Preparation and characterization of a composite PLGA and poly(acryloyl hydroxyethyl starch) microsphere system for protein delivery. Pharmaceutical Research. 2001;18(11):1600–1606.

  • Davis SS, Illum L. Polymeric microspheres as drug carriers. Biomaterials. 1988;9(1):111–115.

  • Ritschel WA. Biopharmaceutic and pharmacokinetic aspects in the design of controlled release peroral drug delivery systems. Drug Development and Industrial Pharmacy. 1989;15:1073–1103.

  • Tripathi KD. Essentials of Medical Pharmacology. New Delhi, India: Jaypee Brothers’ Medical Publishers (P) Ltd; 2007.

  • Martin AR. Antiviral Agents; Text Book of Organic Chemistry and Pharmaceutical Chemistry. New York, NY, USA: Lippincot-Reven; 1998.

  • Lewis GA, Mathieu D, Phan-Tan-Luu R. Pharmaceutical Experimental Design. New York, NY, USA: Marcel Dekker; 1961.

  • Singh B, Ahuja N. Book Review on Pharmaceutical experimental Design. 1999.

  • Nelson KG, Wang LY. Determination of time course of tablet disintegration II: method using continuous functions. Journal of Pharmaceutical Sciences. 1978;67(1):86–89

  • Singh B, Dahiya M, Saharan V, Ahuja N. Optimizing drug delivery systems using systematic ‘design of experiments.’ Part II: retrospect and prospects. Critical Reviews in Therapeutic Drug Carrier Systems. 2005;22(3):215–293.

  • Singh B, Mehta G, Kumar R, Bhatia A, Ahuja N, Katare OP. Design, development and optimization of nimesulide-loaded liposomal systems for topical application. Current Drug Delivery. 2005;2(2):143–153.

  • Aberturas MR, Molpeceres J, Guzmán M, García F. Development of a new cyclosporine formulation based on poly(caprolactone) microspheres. Journal of Microencapsulation. 2002;19(1):61–72.

  • Kim CK, Kim MJ, Oh KH. Preparation and evaluation of sustained release microspheres of terbutaline sulfate. International Journal of Pharmaceutics. 1994;106(3):213–219.


Abstract Views: 136

PDF Views: 0




  • Formulation and Evaluation of Sustained Release Stavudine Microspheres by Ionotropic Gelation Method

Abstract Views: 136  |  PDF Views: 0

Authors

Ayanam Vasavi
Department of Pharmaceutics, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh, India
Miriyala Mrunalini
Department of Pharmaceutics, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh, India
Ayanam Vasanthi
Department of Pharmaceutics, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh, India
G. Raveendra Babu
Department of Pharmaceutical Analysis, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh, India
M. Sowjanya
Department of Chemistry, Vijaya Teja Degree College, Addanki - 523201, Andhra Pradesh, India

Abstract


As a novel drug delivery system, microspheres improve the efficacy of a drug, increase the time of action, lower the number of times in which a dosage form needs to be administered, and to increase patient compliance. Oral administration side effects such as gastric irritation are lessened through the use of microspheres. Ionotropic gelation was used to create HPMC K15M, Guar gum, and Carbopol 934 microspheres with different concentrations of Carbopol 934 polymer. Cross-linking was accomplished with the use of calcium chloride. In order to conduct a systematic evaluation of all the preparations, we performed various tests: morphology, FTIR, DSC, entrapment efficiency, size, microsphere size, and in-vitro drug release. The discrete, free-flowing, and spherical particles of prepared Stavudine microspheres were found. In compliance with standards, the mean particle size was in the range of 72.64 to 95.22 percent. In vitro drug release studies were performed in phosphate buffer solution with a pH of 6.8. As the concentration of sodium alginate and calcium chloride increased, the percentage of drug release was reduced. In the case of F9 formulation, which contained Stavudine, the decreased drug release rate was obtained via carbopol 934(1:3), sodium alginate, and calcium chloride. Conclusively, the present study shows that Stavudine microsphere preparation and formulation F9 are successful. Stavudine microspheres must be prepared in order to preserve an effective drug concentration in serum for a long time, while reducing gastrointestinal irritation.

Keywords


Microspheres, Controlled Release, Stavudine, In-vitro Studies

References