x Acta Scientific | International Open Library | Open Access Journals Publishing Group

Acta Scientific Pharmaceutical Sciences (ASPS)(ISSN: 2581-5423)

Research Article Volume 4 Issue 11

Formulation and Characterization of Albumin/Glycine Microspheres as Oral Delivery System for Resveratrol

Kwame G Yeboah1* and Aladin Siddig2

1College of Pharmacy, Harding University, Searcy, USA
2School of Pharmacy, University of Charleston, USA

*Corresponding Author: Kwame G Yeboah, College of Pharmacy, Harding University, Searcy, USA.

Received: September 22, 2018; Published: October 08, 2020

×

Abstract

Purpose: Resveratrol has been reported to have beneficial effect against many diseases and has multi-spectrum therapeutic applications. However, oral delivery in its free form has short biological half-life with the consequent reduced bioavailability of only one percent. As such, the search continues for a polymer matrix that will be ideal for the protection of the drug and other compounds associated with food system from the conditions encountered in the gastrointestinal tract and to increase therapeutic efficiency.

Purpose of the Study: The purpose of this project therefore, was to evaluate the novel strategy of using albumin and glycine copolymer system to prepare microspheres capable of protecting the Resveratrol and meeting the sustained release specifications for increased bioavailability.

Method: Microspheres containing Resveratrol were prepared using BSA, Glycine and a mixture of BSA/Glycine polymer matrices. The comparative physicochemical characteristics such as particle sizes, zeta potential, drug release, and residual concentration of glutaraldehyde after the crosslinking process for six formulations were evaluated.

Results: The study showed that all the physicochemical characteristics of the selected BSA/Glycine microspheres were ideal for delivery of the resveratrol drug by the oral route. The drug substance was protected at extremely high temperature and oxygen stress. In addition, the residual glutaraldehyde concentrations were below the levels reported to be toxic for peroral delivery. Secondary, a novel means of neutralizing any excess glutaraldehyde by the use of sodium bisulfite was successful incorporated into the formulation.

Conclusion: It was concluded from the results of the study that BSA/Glycine copolymers can be used to produce microspheres with the required specifications for the oral delivery of bioactive compounds such as resveratrol.

Keywords: Resveratrol; Glutaraldehyde; Crosslinking; Glycine; Bioactive Compounds; Microspheres

×

References

  1. Junk K-H., et al. “Resveratrol-loaded polymeric nanoparticles suppress glucose metabolism and tumor growth in vitro and in vivo”. International Journal of Pharmaceutics 478 (2015): 251-257.
  2. Chimento A., et al. “Progress to Improve Oral Bioavailability and Beneficial Effects of Resveratrol”. International Journal of Molecular Science 20 (2019): 1381.
  3. Peng H., et al. “Vanillin cross-linked chitosan microspheres for controlled release of resveratrol”. Food Chemistry 121 (2010): 23-28.
  4. Machado ND., et al. “Resveratrol Recent strategies in Resveratrol delivery systems”. ChemPlusChem 84 (2019): 951-973.
  5. Santos A C., et al. “Nanotechnology-based formulations for resveratrol delivery: Effects on resveratrol in vivo bioavalibility and bioactivity”. Colloids and Surfaces B: Biointerfaces 180 (2019): 127-140.
  6. Andrade S., et al. “Resveratrol brain delivery for neurological disorders prevention and treatment”. Frontiers in Pharmacology 9 (2018): 1261.
  7. Brown V A., et al. “Repeat dose study of the cancer chemopreventive agent resveratrol in healthy volunteers: safety, pharmacokinetics, and effect on the insulin-like growth factor axis”. Cancer Research, 70, 22 (2010): 9003-9011.
  8. Davidov-Pardo G and McClememts D J. “Nutraceutical delivery systems: resveratrol encapsulation in grape see oil nanoemulsions formed by spontaneous emulsification”. Food Chemistry 167 (2015): 205-212.
  9. Radko Y., et al. “Semi-preparative isolation of dihydroresveratrol-3-beta-d-glucuronide and four resveratrol conjugates from human urine after oral intake of resveratrol-containing dietary supplement”. Journal of Chromatography B 930 (2013): 54-61.
  10. Chung I-M., et al. “Resveratrol Nanoparticles: A promising therapeutic advancement over native resveratrol”. Process 8 (2020): 458.
  11. Zhao J., et al. “Improvement strategies for the oral bioavailability of poorly water-soluble flavonoids: An overview”. International Journal of Pharmaceutics 570 (2019): 118642.
  12. Yeboah KG and D’Souza M J. “Evaluation of Albumin microspheres as oral delivery system for Mycobacterium tuberculosis vaccines”. Journal of Microencapsulation2 (2009): 166-179.
  13. Siddig A., et al. “Formulation and characterization of novel riboflavin containing albumin/glycine microspheres”. International Journal of Pharmacy and Integrated Life Sciences10 (2013): 1-25.
  14. Galindo-Rodriquez S A., et al. “Comparative scale-up of three methods for producing ibuprofen-loaded nanoparticles”. European Journal of Pharmaceutical Sciences 25 (2005): 357-367.
  15. Sinha V R and Trehan A. “Biodegradable microspheres for protein delivery”. Journal of Controlled Release 90 (2003): 261-280.
  16. Liu Y Gao., et al. “Α-Lactalbumin and chitosan core-shell nanoparticles: resveratrol loading, protection, and antioxidant activity”. Food and Function 11 (2020): 1525-1536.
  17. Pantusa M., et al. “Stability of trans-Resveratrol associated with transport protein”. Journal of Agriculture and Food Chemistry 62 (2014): 4384-4391.
  18. Lui Y., et al. “Enhanced pH and thermal stability, solubility and antioxidant activity of resveratrol by nanocomplexation with alpha-lactalbumin”. Food and Function 9 (2018): 4781-4790.
  19. Thakkar H., et al. “Albumin microspheres as carriers for the antiarthritic drug celecoxib”. AAPS PharmSciTech 6 (2005): E65-E73.
  20. Bernard N G., et al. “Distribution and degradation of 1-125 albumin microspheres and technetium 99m sulphur colloid”. Journal of Pharmaceutical Sciences, 15 (1980): 30-34.
  21. Miles A P., et al. “Montanide ISA 720 vaccines: quality control of emulsions, stability of formulated antigens, and comparative immunogenicity of vaccine formulations”. Vaccine 19 (2005): 2530-2539.
  22. Ogienko A G., et al. “Large porous particles for respiratory drug delivery. Glycine-based formulations”. European Journal of Pharmaceutical Sciences 110 (2017): 148-156.
  23. Zhu D., et al. “Long term stability of a recombinant Plasmodium falciparum AMA1 malaria vaccine adjuvanted with Montanide ISA 720 and stabilized with glycine”. Vaccine 29 (2011): 3640-3645.
  24. Papageorgiou G C and Murata N. “The unusually strong stabilizing effects of glycine betaine on the structure and function of the oxygen-evolving Photosystem II complex”. Photosynthesis Research 44 (1995): 243-252.
  25. Kasraian K., et al. “Characterization of the Sucrose/Glycine/Water system by Differential Scanning Calorimetry and freeze-drying microscopy”. Pharmaceutical Development and Technology2 (1998): 233-239.
  26. Adesunloye T A and Stach PE. “Effect of Glycine/Citric acid on the dissolution stability of hard gelatin capsules”. Drug Development and Industrial Pharmacy6 (1998): 493-500.
  27. Silva C J S M., et al. “Chemical modification on proteins using glutaraldehyde”. Food technology and Biotechnology1 (2004): 51-56.
  28. Migneualt I., et al. “Glutaraldehyde: behavior in aqueous solution, reaction with proteins, and application to enzyme crosslinking”. Biotechniques5 (2004): 790-802.
  29. Furst W and Banerjee A. “Release of glutaraldehyde from an albumin-glutaraldehyde tissue adhesive causes significant in vitro and in vivo toxicity”. Annals of Thoracic Surgery5 (2005): 1522-1528.
  30. Boratynski J and Zal T. “Colorimetric micro methods for glutaraldehyde determination by means of phenol and sulfuric acid or phenol and perchloric acid”. Analytical Biochemistry2 (1990): 259-262.
  31. Jordan SL., et al. “Inactivation of glutaraldehyde by reaction with sodium bisulfite”. Journal of Toxicology and Environmental Health3 (1996): 299-309.
  32. Trela B C and Waterhouse A L. “Resveratrol: Isomeric molar absorptivities and stability”. Journal of Agricultural and Food Chemistry5 (1996): 1253-1257.
  33. Camont L., et al. “Simple spectrophotometric assessment of the trans-/cis-resveratrol ratio in aqueous solutions”. Analytica Chimica Acta 634 (2009): 121-128.
  34. Ballantyne B and Jordan S L. “Toxicological, medical and industrial hygiene aspects of glutaraldehyde with particular reference to its biocidal use in cold sterilization procedures”. Journal of Applied Toxicology2 (2001): 131-151.
  35. Ballantyne B and Myers RC. “The acute toxicity and primary irritancy of glutaraldehyde solutions”. Veterinary and Human Toxicology4 (2001): 193-202.
  36. Galindo-Rodriquez S A., et al. “Polymeric nanoparticles for oral delivery of drugs and vaccines: A critical evaluation of in vivo studies”. Critical Review in Therapeutics Drug Carrier Systems5 (2005): 419-463.
  37. Prinn K B., et al. “Statistical modeling of protein spray drying at the laboratory scale”. AAPS PharmSciTech1 (2002): 1-8.
  38. Leach W T., et al. “Encapsulation of protein nanoparticles into uniform-sized microspheres formed in a spinning oil film”. AAPS PharmSciTech 6 (2005): 605-617.
  39. Cho A R., et al. “Preparation of chitosan-TPP microspheres as resveratrol carriers”. Journal of Food Science4 (2014): E568-E576.
  40. Das S and Ng K Y. “Resveratrol loaded calcium-pectinate beads: effects of formulation parameters on drug release and bead characteristics”. Journal of Pharmaceutical Sciences2 (2010): 840-860.
  41. Ko JA., et al. “Preparation and characterization of chitosan microparticles intended for controlled drug delivery”. International Journal of Pharmaceutics 249 (2002): 165-174.
  42. Muller BG., et al. “Albumin nanospheres as carriers for passive drug targeting: An optimized manufacturing technique”. Pharmaceutical Research 13 (1996): 32-37.
  43. Luftensteiner CP and Viernstein H. “Statistical experimental design based studies on placebo and mitoxantrone-loaded albumin microspheres”. International Journal of Pharmaceutics 171 (1998): 87-99.
  44. El-Mahdy M., et al. “Effects of preparation conditions on the monodispersity of albumin microspheres”. Journal of Microencapsulation 15 (1998): 661-673.
  45. Norris A and Sinko P. “Effect of size, surface charge, and hydrophobicity on the translocation of polystyrene microspheres through gastrointestinal mucin”. Journal of Applied Polymer Science 63 (1998): 1481-1492.
  46. Danaei M., et al. “Impact of particle size and Polydispersity Index on the clinical applications of lipidic nanocarrier systems”. Pharmaceutics57 (2018): 1-17.
  47. Ahsan F., et al. “Targeting to macrophages: role of physicochemical properties of particulate carrier-liposomes and microspheres-on the phagocytosis by macrophages”. Journal of Controlled Release 79 (2002): 29-40.
  48. De Cassia da Silva R., et al. “Resveratrol: a thermoanalytical study”. Food Chemistry 237 (2017): 561-565.
  49. Davidov-Pardo G., et al. “Resveratrol encapsulation: Designing delivery systems to overcome solubility, stability and bioavailability issues”. Trends in Food Science and Technology 38 (2014): 88-103.
  50. Amri A., et al. “Administration of resveratrol: What formulation solutions to bioavailability limitations?” Journal of Controlled Release 158 (2012): 182-193.
×

Citation

Citation: Kwame G Yeboah and Aladin Siddig. “Formulation and Characterization of Albumin/Glycine Microspheres as Oral Delivery System for Resveratrol". Acta Scientific Pharmaceutical Sciences 4.11 (2020): 14-29.




Metrics

Acceptance rate32%
Acceptance to publication20-30 days
Impact Factor0.759

Indexed In




News and Events


  • Certification for Review
    Acta Scientific certifies the Editors/reviewers for their review done towards the assigned articles of the respective journals.
  • Submission Timeline for Upcoming Issue
    The last date for submission of articles for regular Issues is July 30, 2021.
  • Publication Certificate
    Authors will be issued a "Publication Certificate" as a mark of appreciation for publishing their work.
  • Best Article of the Issue
    The Editors will elect one Best Article after each issue release. The authors of this article will be provided with a certificate of “Best Article of the Issue”.
  • Welcoming Article Submission
    Acta Scientific delightfully welcomes active researchers for submission of articles towards the upcoming issue of respective journals.
  • Contact US