Optimization of formulation processes using Design Expert® Software for preparation of polymeric blends-artesunate-amodiaquine HCl microparticles

作者: John Dike N. Ogbonna , Anthony A. Attama , Kenneth C. Ofokansi , Sanjay B. Patil , Ganesh D. Basarkar

DOI: 10.1016/J.JDDST.2017.02.011

关键词: Differential scanning calorimetryPolymer blendGlutaraldehydeMaterials scienceFactorial experimentDispersityPolymer chemistryCrystallinityDesign–ExpertParticle sizeChemical engineering

摘要: Abstract A 2 3 Factorial design of cissus-gelatin B polymer blends was developed to formulate amodiaquine HCl-artesunate (AQ-AS) microparticles by varying the blend concentration (2 %w/v, 5 %w/v), crosslinking time (0.5 h, 1 h) and glutaraldehye volume (0.5 ml, 1 ml). The formulations were evaluated using drug entrapment efficiency (EE), particle size, polydispersity index, thermal behavior with differential scanning calorimetry, crystallinity powder X-ray diffraction, morphology electron microscope in vitro release combination simulated gastric fluid (SGF, pH = 7.4, 95%) methanol (5%). expected responses, EE fitted into Design Expert ® . exhibited pseudoplastic there no marked change in rheology 2% w/v dispersion at 55 °C. AQ-AS formulated dark brownish discrete mass, physically stabilized, irregular shape, polydisperse, partially crystalline system. An optimal formulation comprising (5 glutaraldehyde (1 ml) cross-linking (0.5 h) identified provide desired values for EE, amodaquine HCl (47.41%), artesunate (36.42%) release. This study proposes best opportunity selection factors required optimum drugs.

参考文章(41)
Yongqiang Li, Mohammadreza R. Abbaspour, Paul V. Grootendorst, Andrew M. Rauth, Xiao Yu Wu, Optimization of controlled release nanoparticle formulation of verapamil hydrochloride using artificial neural networks with genetic algorithm and response surface methodology European Journal of Pharmaceutics and Biopharmaceutics. ,vol. 94, pp. 170- 179 ,(2015) , 10.1016/J.EJPB.2015.04.028
Bing Gu, Brian Linehan, Yin-Chao Tseng, Optimization of the Büchi B-90 spray drying process using central composite design for preparation of solid dispersions. International Journal of Pharmaceutics. ,vol. 491, pp. 208- 217 ,(2015) , 10.1016/J.IJPHARM.2015.06.006
Sabinus I. Ofoeful and Anthony A. Attama, Biopolymer Blends: Applications, Limitations, and Future Prospects ,(2009)
John D. N Ogbonna, Franklin C. Kenechukwu, Chinekwu S. Nwobi, Onochie S. Chibueze, Anthony A. Attama, Formulation,in vitroandin vivoevaluation of halofantrine-loaded solid lipid microparticles Pharmaceutical Development and Technology. ,vol. 20, pp. 941- 948 ,(2015) , 10.3109/10837450.2014.949270
Oluwatosin G. Tade, Seun F. Akomolafe, Ganiyu Oboh, Afolabi A. Akindahunsi, Ayodele J. Akinyemi, Inhibitory Effect of Aqueous Extract of Stem Bark of Cissus populnea on Ferrous Sulphate- and Sodium Nitroprusside-Induced Oxidative Stress in Rat’s Testes In Vitro International Scholarly Research Notices. ,vol. 2013, pp. 130989- 130989 ,(2013) , 10.1155/2013/130989
Sanjay B Patil, Krutika K Sawant, None, Development, optimization and in vitro evaluation of alginate mucoadhesive microspheres of carvedilol for nasal delivery. Journal of Microencapsulation. ,vol. 26, pp. 432- 443 ,(2009) , 10.1080/02652040802456726
Niesko Pras, Jan F. Visser, Sieb Batterman, Herman J. Woerdenbag, Theo M. Malingré, Charles B. Lugt, Laboratory selection of Artemisia annua L. for high artemisinin yielding types Phytochemical Analysis. ,vol. 2, pp. 80- 83 ,(1991) , 10.1002/PCA.2800020208
Sachin Gahoi, Gaurav K Jain, Renu Tripathi, Swaroop K Pandey, Mohammed Anwar, Musarrat H Warsi, Mayank Singhal, Roop K Khar, Farhan J Ahmad, None, Enhanced antimalarial activity of lumefantrine nanopowder prepared by wet-milling DYNO MILL technique. Colloids and Surfaces B: Biointerfaces. ,vol. 95, pp. 16- 22 ,(2012) , 10.1016/J.COLSURFB.2012.01.047
Ashish K Mehta, Khushwant S Yadav, Krutika K Sawant, None, Nimodipine loaded PLGA nanoparticles: formulation optimization using factorial design, characterization and in vitro evaluation. Current Drug Delivery. ,vol. 4, pp. 185- 193 ,(2007) , 10.2174/156720107781023929