Design, development and optimization of carvedilol microspheres using 32 factorial design

Paper Details

Research Paper 13/05/2024
Views (539)
current_issue_feature_image
publication_file

Design, development and optimization of carvedilol microspheres using 32 factorial design

Aisha Rahman, K. Latha, Aymen Fatima, Vyshak R. Menon, T. Shailaja
J. Biodiv. & Environ. Sci. 24(5), 140-152, May 2024.
Copyright Statement: Copyright 2024; The Author(s).
License: CC BY-NC 4.0

Abstract

Carvedilol being a BCS class II drug has low solubility and it has short half-life of 2-6 hrs. The objective of the study is to design, develop and optimize carvedilol microspheres using factorial design. Solubility was enhanced by formulating into solid dispersion using solvent evaporation technique and solid dispersion with enhanced solubility was incorporated into sodium alginate microspheres prepared by ionic gelation method and were optimized by 3-level, 2-factor full factorial design. Solid dispersion formulation SD3 showed 15.3 folds enhanced solubility compared to the pure drug. Powder X-ray Diffractogram patterns revealed that the crystalline drug was transformed into an amorphous form. SD3 formulation was incorporated into sodium alginate microspheres and the microspheres were optimized. The optimized microsphere formulation had an entrapment efficiency of 79.41% and showed 80% drug release at 6 hrs. Scanning electron microscopic images proved, that optimized microspheres were spherical in shape and had rough surface.

Adepu S, Ramakrishna S. 2021. Controlled drug delivery systems: Current status and future directions. Molecules 26(19), 5905.

Chein YW. 1992. Novel drug delivery systems. Marcel Dekker Inc., New York, 13.

Chhater S, Praveen K. 2013. Solid Dispersion Incorporated Microcapsules: Predictive Tools for Improve the Half Life and Dissolution Rate of Pioglitazone Hydrochloride. American Journal of Biomedical Research 1(3), 57-70. DOI: 10.12691/ajbr-1-3-3.

Gadad AP, Naik SS, Dandagi PM, Bolmal UB. 2016. Formulation and evaluation of gastroretentive floating microspheres of lafutidine. Indian Journal of Pharmaceutical Education and Research 50(2), S76-S81. DOI: 10.5530/ijper.50.2.21

Kshirsagar SJ, Patil SV, Bhalekar MR. 2011. Statistical optimization of floating pulsatile drug delivery system for chronotherapy of hypertension. International journal of pharmaceutical investigation 1(4), 207–213. https://doi.org/10.4103/2230-973X.93005

Manubolu K, Sujatha B, Sreenivasulu M, Kumar SR, Kumar SN, Rao KB. 2015. Formulation and in vitro evaluation of gliclazide microbeads. World Journal of Pharmaceutical Research 4(5), 1970-1982.

Meshram BMS, Mishra A, Pathak A. 2016. Formulation and Evaluation of Microsphere of Rabeprazole Sodium. International Journal of Advances in Pharmaceutics 5(3), 76-83. DOI: 10.7439/ijap

Miyazaki S, Aoyama H, Kawasaki N, Kubo W, Attwood D. 1999. In situ-gelling gellan formulations as vehicles for oral drug delivery. Journal of Controlled Release 60(2), 287–295. DOI: 10.1016/S0168-3659(99)00084-X

Miyazaki S, Kawasaki N, Kubo W, Endo K, Attwood D. 2001. Comparison of in situ gelling formulations for the oral delivery of cimetidine. International journal of pharmaceutics 220(1-2), 161–168. https://doi.org/10.1016/s0378-5173(01)00669-x

Patil SV, Lade PD, Janugade BU, Babar SA, Ghewade YB. 2009. Effect of Concentration of Gellan Gum and Calcium Chloride Solution on Entrapment Efficiency and Drug Release from Calcium Gellan Beads. Research Journal of Pharmacy and Technology 2(4), 862-865.

Kumar KR, Suresh G. 2018. Development and characterization of alginate microspheres containing olmesartan by ionotropic gelation method. International Journal of Pharmaceutical Science and Drug Research 10(4), p.335-341. DOI: 10.25004/IJPSDR.2018.100420

Remington JP. 2021. Remington: The science and practice of pharmacy (Vol. 1). Lippincott Williams & Wilkins.

Sharma A, Jain CP. 2010. Preparation and characterization of solid dispersions of carvedilol with PVP K30. Research in Pharmaceutical Sciences 5(1), 49–56.

Siddiqui MN, Garg G, Sharma PK. 2011. A Short Review on ‘A Novel Approach in Oral Fast Dissolving Drug Delivery System and Their Patents’. Advances in Biological Research 5(6), 291-303.

Sompur CK, Doijad RC, Patil SM, Maske AP. 2011. An approach for development of oral sustained release suspension. International Journal of Pharma and Bio Sciences 2(2), 320–329.

Verma P, Thakur AS, Deshmukh K, Jha AK, Verma S. 2010. Routes of drug administration. International Journal of Pharmaceutical Studies and Research 1(1), 54-59.

Yuvaraja K, Khanam J. 2014. Enhancement of carvedilol solubility by solid dispersion technique using cyclodextrins, water soluble polymers and hydroxyl acid. Journal of Pharmaceutical and Biomedical Analysis 96, 10-20. DOI: 10.1016/j.jba.2014.03.019.

Related Articles

Evaluating curriculum alignment, accuracy, and readability of ‘environmental disaster, sanitation, and waste management

Analyn I. Diola*, Priscilla R. Castro, J. Biodiv. & Environ. Sci. 28(2), 1-11, February 2026.

Above and below ground carbon stock assessment of natural and planted mangrove forest in Davao Occidental, Philippines

C. F. Mangaga*, W. T. Tatil, H. A. R. Quiaoit, P. D. Suson, J. Biodiv. & Environ. Sci. 28(1), 157-167, January 2026.

Extraction and characterization of distilled water from by-product of salt refinery processing

Analyn I. Diola*, Eric A. Cunanan, Irene A. De Vera, Christian Garret F. Aquino, Julie M. Agpaoa, J. Biodiv. & Environ. Sci. 28(1), 151-156, January 2026.

Vulnerability to illegal, unreported and unregulated (IUU) fishing: The case of the Talusan, Zamboanga Sibugay, Philippines

Angelica M. Darunday*, Judy Ann H. Fernandez, Shekinah L. Ogoc, Norlika D. Moti, Larry C. Herbito, Armi G. Torres, J. Biodiv. & Environ. Sci. 28(1), 138-150, January 2026.

Socio-ecological dimensions of intertidal gleaning: The use of local ecological knowledge to identify commercially important gastropods in Iligan Bay, Philippines

Katrina Flores, Armi G. Torres, Wella T. Tatil, Ivane R. Pedrosa-Gerasmio*, J. Biodiv. & Environ. Sci. 28(1), 126-137, January 2026.

Conservation assessment of the marine ornamental fish species Pomacanthus imperator (Emperor angelfish) in the Philippines

Timothy Jan L. Adel*, Armi G. Torres, J. Biodiv. & Environ. Sci. 28(1), 114-125, January 2026.

Land use conflicts: An impediment to improved agrifood value chain management as perceived by crop farmers in southeast Nigeria

J. U. Chikaire, C. C. Ejiogu, H. I. Duruanyim, T. O. Ogbuji, S. I. Ogbaa, A. O. Kalu, J. I. Ukpabi, A. Rufai, L. C. Izunobi, J. U. Okwudili, C. I. Anah, E. U. Omeire, I. O. Okeoma, J. Nnametu, U. G. Chris-Ejiogu, I. E. Edom, C. N. Atoma, U. S. Awhareno, E. C. Mube-Williams, S. O. Adejoh, A. D. Ude, J. O. Oparaojiaku, C. O. Osuagwu, E. E. Ihem, B. N. Aririguzo, E. C. C. Amaechi, M. N. Osuji, C. A. Acholonu, J. Biodiv. & Environ. Sci. 28(1), 102-113, January 2026.