IN VITRO PROPERTIES OF SOLID LIPID MICROPARTICLES (SLMS) LOADED WITH METHANOLIC EXTRACT OF GARCINIA KOLA (HECKEL) SEED
Objective: The decline in the use of herbal medicine especially in the Western world may be due to lack of readily available market brand formulations and the fact that most herbal remedies are taken as tea, decoctions and infusions. The taste of some of these herbal drugs is not palatable, and some have unpleasant odour and colour hence, the need to formulate these drugs in form of encapsulated dosage forms. The objective of the work was to formulate solid lipid microparticles (SLMs) loaded with the methanolic extract of Garcinia kola seed.
Methods: The SLMs containing 1 and 3 % of Garcinia kola seed extract were formulated using fat from Capra hircus and PhospholiponÂ® 90H (3:1). The particle morphology and size, encapsulation efficiency (EE%), pH, in vitro release and the inhibition zone diameter (IZD) of the SLMs were determined.
Results: The results showed that the extract was very bitter while, the encapsulated G. kola had slight bitter taste. The pH remained in the acidic region from 1 to 30 days. Particle size of 28.65 Â± 1.13 and 29.49 Â± 1.24 Âµm were obtained for SLMs loaded with 1 and 3 % of the extract respectively. SLMs had high EE% of 94 % and also exhibited good release of the extract in simulated intestinal fluid (SIF, pH 7.2). Garcinia kola-loaded SLMs had good activity against Staphylococcus aureus and no action against Escherichia coli.
Conclusion: Therefore, Garcinia kola seed extract could be formulated as SLMs in order to mask its bitter taste and improve compliance.
2. Majekodunmi SO, Adegoke OA, Odeku OA. Formulation of the extract of the stem bark of Alstonia boonei as tablet dosage form. Trop J Pharm Res 2008;7 (2): 987-994.
3. Chime SA, Ugwuoke CEC, Onyishi VI, et al. Formulation and evaluation of Cymbopogon citratus dried leaf-powder tablets. Afri J Pharm Pharmacol 2012;6(48): 3274-3279.
4. Chime SA, Brown SA, Ugwu CE, et al. Effect of binder type and concentration on the in vitro properties of Alstonia boonei tablets. Int J Pharm Sci Rev Res 2012;16(2):5-9.
5. Chime SA, Attama AA, Builders PF, et al. Sustained release diclofenac potassium-loaded solid lipid microparticle based on solidified reverse micellar solution: In vitro and in vivo evaluation. J Micro. 2012: 1â€“11. DOI: 10.3109/02652048.2012.726284.
6. Eradel MS, Gugor S, Ozsoy Y et al. Preparation and in vitro evaluation of indomethacin loaded solid lipid microparticles. Acta Pharm Sci 2009;51:203-210.
7. Milak S, Medicott N and Tucker IG. Solid lipid micro particles containing loratidine prepared using a micro mixer. J Micro 2006;23:823â€“831.
8. Fricker G, Kromp T, Wendel A, et al. Phospholipids and lipid-based formulations in oral drug delivery. Pharm Res 2010;27:1469-1486.
9. Obitte NC, Chime SA, Magaret AA, et al. Some in vitro and pharmacodynamic evaluation of indomethacin solid lipid microparticles. Afr J Pharm Pharmcol 2012;6(30):2309-2317.
10. Ndukwe KC, Okeke IN, Lamikanra A, et al. Antibacterial activities of aqueous extracts of selected chewing sticks. J Contemp Dent Pract 2005;3:86-94.
11. Iwu MM. Handbook of African medicinal Plants. Boca Raton: CRC Press Inc. 1993, 223-224.
12. Adesina SK, Gbile ZO, Odukoya OA, et al. Survey of indigenous useful plants of West Africa with special emphasis on medicinal plants and issues associated with management. The United Nations Programme on Natural Resources in Africa; 2nd edition, 1995, 84-85.
13. Adegboye MF, Akinpelu DA, Okoh AI. The bioactive and phytochemical properties of Garcinia kola (Heckel) seed extract on some pathogens. Afr J Biotech 2008;7(21):3934-3938.
14. Ayensu ES. Medicinal Plants of West Africa, Reference Publ. Inc., Algonac, Michigan. 1978, 162.
15. Ajebesone PE, Aina JO. Potential African Substances for Hops in Tropical Beer Brewing. J Food Technol Afr. 2004;9(1):13-16.
16. Akpantah AO, Oremosu AA, Noronha CC, et al. Effects of Garcinia kola seed extract on ovulation, oestrous cycle and foetal development in cyclic female Sprague - Dawley rats. Nigerian J Physio Sci 2005;20(1-2):58-62.
17. Gaytan E, Trrradas E, Morales C, et al. Morphorlogical evidence for uncontrolled proteolytic activity during the ovulatory process in indomethacin treated rats. Reprod 2002;123:639-649.
18. Onunkwo GC, Egeonu HC, Adikwu MU, et al. Some Physical Properties of tabletted seed of Garcinia kola (Heckel). Chem Pharm Bull 2004;52:649-653.
19. Okoko T. In vitro antioxidant and free radical scavenging activities of Garcinia kola seeds. Food Chem Toxicol. 2009;47(10):2620-2623.
20. Okunji C, Komarnytsky S, Fear G, et al. Preparative isolation and identification of tyrosinase inhibitors from the seeds of Garcinia kola by high-speed countercurrent chromatography. J Chromatog 2007;1151:45-50.
21. Han QB, Lee S, Qiao CF, et al. Complete NMR assignments of the bntibacterial Biflavonoid GB1 from Garcinia kola. Chem Pharm Bull 2005;53:1034-1036.
22. Owoseni A, Ogunnusi T. Antibacterial effects of three chewing stick extracts on Lactobacillus species. Int J Trop Med 2006;3:103-106.
23. Ogbulie JN, Ogueke CC, Nwanebu FC. Antibacterial properties of Uvaria chamae, Congronema latifolium, Garcinia kola, Vernonia amygdalina and Aframomium melegueta. Afr J Biotech 2007;6:1549-1553.
24. Brown SA, Chime SA, Attama AA, et al. In vitro and in vivo characterisation of piroxicam-loaded dika wax lipospheres. Trop J Pharm Res. 2013, 12 (1): 33-38.
25. Attama AA, Okafor CE, Builders PF, et al. Formulation and in vitro evaluation of a PEGylated microscopic lipospheres delivery system for ceftriaxone sodium. Drug Deliv 2009;16:448â€“616.
26. Umeyor EC, Kenechukwu FC, Ogbonna JD, et al. Preparation of novel solid lipid microparticles loaded with gentamicin and its evaluation in vitro and in vivo. J Micro. 2012:1- 12. DOI: 10.3109/02652048.2011.651495.
27. Hassan MA, Mohammed FA, Sabour EA. Formulation and evaluation of ciprofloxacin hydrochloride and norfloxacin gel. STP Pharma Sci 2003;13:195â€“201.
28. Khopade AJ, Jain NK. Long circulating lipospheres targeted to inflamed tissue. Pharmazie 1997;52:165-166.
29. Chime SA, Attama AA, Onunkwo GC. Sustained release indomethacin-loaded solid lipid microparticles, based on solidified reverse micellar solution (SRMS): in vitro and in vivo evaluation. J Drug Del Sci Tech 2012;22(5):485-492.