Development of Theophylline Microbeads Using PregelatinizedBreadfruit Starch (Artocarpus altilis) as a Novel Co-polymer for Controlled Release

Abstract

Purpose: The aim of this study was to prepare formulations of theophylline microbeads usingpregelatinized breadfruit starch (Artocarpus altilis, family Moraceae) in combination withsodium alginate and chitosan at various polymer: drug ratios. Microbead formulations forcontrolled delivery of theophylline would be better alternatives to conventional dosage formsfor optimized drug therapy.Methods: The native and pregelatinized starches were characterized for morphology (scanningelectron microscope), crystallinity (Fourier transform intra-red spectroscopy, FTIR and X-raydiffractometer, XRD), thermal flow (differential scanning colorimeter), density and flowproperties. Theophylline microbeads were prepared by ionic gelation and characterized usingsize, swelling index, entrapment efficiency and time required for 15% and 50% drug release (t15and t50 respectively).Results: FTIR and XRD spectra revealed the orderly arrangement of granules of the semi-crystallinebreadfruit starch was disrupted on gelatinization. The viscosity and flow of pregelatinized starchwere enhanced. Theophylline microbeads were near spherical in shape with size range 1.09± 0.672 to 1.58 ± 0.54 mm. FTIR and XRD spectra confirmed there was no drug-polymerinteraction. Microsphere size, swelling increased while entrapment and dissolution time (t50)reduced with polymer: drug ratio. The entrapment efficiency ranged from 30.99 ± 1.32 to 78.50± 2.37%. Optimized formulation, starch: alginate ratio 3:1 at polymer: drug ratio of 2:1, gave aprolonged dissolution time (t50 = 8.40 ± 1.20 h).Conclusion: Breadfruit starch was suitable as a copolymer for the controlled delivery oftheophylline in microbeads which could serve as a substitute to synthetic polymers in drugdelivery.

Influence of Pregelatinized Breadfruit Starch-Alginate Blend as a Sustained Release Polymer in Theophylline Microbeads Using Box Behnken Design

“…The main diffraction peaks were observed to be between 5 and 23° (2θ) angle. The XRD spectrum of the pregelatinized starch confirmed the disruption of the internal order of the native starch granules, resulting in a more amorphous polymer (Okunlola and Adewusi, 2019).…”

“…The native starch had oval-shaped granules with mean size of 8.44 ± 4.00 μm. Modification by pregelatinization produced larger, irregular-shaped starch granules with mean size of 34.45 ± 6.70 μm (Okunlola & Adewusi, 2019). The XRD spectra of the starches are shown in Fig.…”

“…Aqueous slurry of the dry native starch powder was prepared with 100 g of starch powder dispersed in 500 ml of distilled water and then heated at 70°C with constant stirring for 30 minutes. The resulting paste was dried in hot air oven at 50°C for 48 hours and blended into powder (Okunlola and Adewusi, 2019).…”

Central Composite Design Screened Mastic Gum Abetted Mucoadhesive Microspheres of Amoxicillin Trihydrate for Exterminating H. pylori

“…HCl (0.1M) warmed to 37±2°C was applied to the tissue at a rate of 5 ml/min. The time required for detaching all AMMM from the mucosal surface of the sheep stomach by visual inspection (eq.4) [17,18].…”

Specialty Dihydrobenzoxanthone’s Artocarpus Purified By Vacuum Liquid Chromatography (VLC)

“…(ii) Infrared spectrum to know the functional groups. (iii) NMR (Nuclear Magnetic Resonances) is a great tools for determinining of pure compound (Okunlola, 2019).…”