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Research Article Open access CC BY 3.0

Optimization of Gabapentin Release and Targeting Absorption, Through Incorporation into Alginate Beads

Pierre A. Hanna, Shadeed Gad, Hassan M. Ghonaim, Mamdouh M. Ghorab

Journal of Pharmaceutical Research International · pp. 597–616 · Published 24 May 2013

10.9734/BJPR/2013/3020

Abstract

Aims: 1) To study the effect of some formulation variables on drug load, encapsulation efficiency, swelling ratio, mucoadhesion and drug release. 2) Optimize the mucoadhesion capabilities for targeting drug absorption and release-controlling capabilities of alginate beads. Methodology: Alginate beads were prepared by dripping sodium alginate gel into calcium chloride solution and then dried overnight at ambient temperature. The effects of alginate concentration, cross linker concentration, cross linking time, volume of cross linking solution and drug/polymer ratio on drug load, encapsulation efficiency, swelling ratio, mucoadhesion and drug release were investigated. Formulae containing sodium lauryl sulfate (SLS), gabapentin-ethylcellulose solid dispersion, mixture of free drug and solid dispersion were prepared for modifying the drug release rate. Results: Mucoadhesion of alginate beads was shown to be decreased upon adding SLS (30% after 8 hrs). Drug release was so fast (92.46% after 2 hrs). The incorporation of solid dispersion has led to well accepted mucoadhesion (74.44% after 8 hrs) as well as release properties (93.35% after 10 hrs) Beads containing mixtures of drug and ethylcellulose-drug solid dispersion showed acceptable mucoadhesion (74.44% after 8 hrs) and control of gabapentin release (93.35% after 10 hrs). Statistical analysis of variance between groups was performed using the one-way layout ANOVA with duplication. Significant differences in mean values were evaluated by Student's unpaired t test (P < 0.05). Conclusion: A finally optimized formula was suggested by incorporating a combination of solid dispersion and free gabapentin in alginate system to achieve burst release of gabapentin and hence fast effect (33.417% was released during the first 30 minutes in fasting-simulated conditions) and controlled release (91.217% after 6 hrs).

Alginate control release targeting gabapentin sodium lauryl sulfate ethyl cellulose solid dispersion.

References (33)

  1. 1 Statistical Mechanics of Cross-Linked Polymer Networks II. Swelling [DOI]
  2. 2 Alginate in Drug Delivery Systems [DOI]
  3. 3 Investigation of swelling/degradation behaviour of alginate beads crosslinked with Ca2+ and Ba2+ ions [DOI]
  4. 4 Swelling studies and in vitro release of verapamil from calcium alginate and calcium alginate–chitosan beads [DOI]
  5. 5 Semi-interpenetrating polymer network microspheres of gelatin and sodium carboxymethyl cellulose for controlled release of ketorolac tromethamine [DOI]
  6. 6 A Saturable Transport Mechanism in the Intestinal Absorption of Gabapentin Is the Underlying Cause of the Lack of Proportionality Between Increasing Dose and Drug Levels in Plasma [DOI]
  7. 7 Alginate microspheres prepared by internal gelation: Development and effect on insulin stability [DOI]
  8. 8 Xanthan–alginate composite gel beads: Molecular interaction and in vitro characterization [DOI]
  9. 9 Preparation of sodium alginate–methylcellulose blend microspheres for controlled release of nifedipine [DOI]
  10. 10 Combined Physical and Chemical Immobilization of Glucose Oxidase in Alginate Microspheres Improves Stability of Encapsulation and Activity [DOI]
  11. 11 Intestinal transit of bioadhesive microspheres in an in situ loop in the rat—A comparative study with copolymers and blends based on poly(acrylic acid) [DOI]
  12. 12 Effect of compaction pressure on the dissolution efficiency of some direct compression systems.
  13. 13 Controlling of systemic absorption of gliclazide through incorporation into alginate beads [DOI]
  14. 14 Bioadhesive microspheres: I. A novel electrobalance-based method to study adhesive interactions between individual microspheres and intestinal mucosa [DOI]
  15. 15 Encapsulation of recombinant adenovirus into alginate microspheres circumvents vector-specific immune response [DOI]
  16. 16 Formulation and investigation of nicardipine HCl–alginate gel beads with factorial design-based studies [DOI]
  17. 17 Design and Development of Gliclazide Mucoadhesive Microcapsules: In Vitro and In Vivo Evaluation [DOI]
  18. 18 Alginate microparticles as novel carrier for oral insulin delivery [DOI]
  19. 19 Oral controlled release of melatonin using polymer-reinforced and coated alginate beads [DOI]
  20. 20 Interaction of calcium-induced alginate gel beads with propranolol. [DOI]
  21. 21 Sodium lauryl sulfate impedes drug release from zinc-crosslinked alginate beads: Switching from enteric coating release into biphasic profiles [DOI]
  22. 22 Biological evaluation of calcium alginate microspheres as a vehicle for the localized delivery of a therapeutic enzyme [DOI]
  23. 23 Formulation and Evaluation of Oral Mucoadhesive Multiparticulate System Containing Metoprolol Tartarate: An In Vitro – Ex Vivo Characterization [DOI]
  24. 24 Cloning of Pseudomonas aeruginosa algG, which controls alginate structure [DOI]
  25. 25 Effect of gelation conditions and dissolution media on the release of paracetamol from alginate gel beads [DOI]
  26. 26 Cross-Protective Immunity of Mice Induced by Oral Immunization with Pneumococcal Surface Adhesin A Encapsulated in Microspheres [DOI]
  27. 27 Gabapentin dosing in the treatment of epilepsy [DOI]
  28. 28 Stability Studies of Gabapentin in Aqueous Solutions [DOI]
  29. 29 Development of calcium alginate -gelatin based microspheres for controlled release of endosulfan as a model pesticide
  30. 30 Evaluation of diltiazem hydrochloride-loaded mucoadhesive microspheres prepared by emulsification-internal gelation technique.
  31. 31 Bioadhesive microspheres: III. An in vivo transit and bioavailability study of drug-loaded alginate and poly(fumaric-co-sebacic anhydride) microspheres [DOI]
  32. 32 Development of a system for simultaneous dissolution studies and magnetic resonance imaging of water transport in hydrodynamically balanced systems: A technical note [DOI]
  33. 33 Biodegradable alginate microspheres as a delivery system for naked DNA.

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