• Salome Amarachi Chime


To formulate artemether lumefantrine loaded lipospheres and to evaluate the effect of excipients on the in vitro properties



Materials and methods: Lipospheres were formulated using goat fat (70 percentage) and Phospholipon 90H (70 percentage) as the lipid matrix, Solutol HS 15 and Soluplus were used respectively as surfactants.  The lipospheres were formulated by melt homogenization and analysed for drug content, encapsulation efficiency (EEpercentage), particle size and pH stability. In vitro release was studied in simulated gastric fluid (SGF, 1.2) and simulated intestinal fluid (SIF, 7.2).       Results: Lipospheres formulated with Solutol had particle size range of 24.16 to 30.89 μm, while those formulated with Soluplushad particle size range of 24.72 to 74.16 μm. The formulations showed a decline in pH at 30 days. The EE of artemether range from 71.80 to 75.30 percentage for lipospheres formulated with Soluplus, while those formulated with Solutolhad EEpercentage of 65.30 to 75.02 percentage. Also, the EEpercentage of lumefantrine ranged from 76.36 to 88.99 percentage for lipospheres formulated with Soluplus, while those containing Solutolhad EE range of 73.22 to 85.06 percentage. Formulations exhibited sustained release properties with maximum release of at 6 h, however, lumefantrine exhibited higher release than artemether in SIF (p less than 0.05) and significantly lower release in SGF (p less than 0.05).                                                                                                                                           Conclusion: Lipospheres exhibited good properties as a delivery system for artemether-lumefantrine.


Keywords: Goat fat, phospholipid, antimalaria, melt homogenization, loading capacity


1. Santos-Magalhaes NS, Mosqueira VCF. Nanotechnology applied to the treatment of malaria. Adv Drug Deliv Rev 2010; 62:560-575.

2. Afonso A, Hunt P, Cheesman S, Alves AC, Cunha CV, de Rosario V, Cravo P. Malaria parasites can develop stable resistance to artemisinin but lack mutations in candidate genes atp6 (encoding the sarcoplasmic and endoplasmic reticulum Ca2+ ATPase), tctp, mdr1, and cg10. Antimicrob Agents Chemother 2006; 50:480-488.

3. Puri SK, Chandra R. Plasmodium vinckei: Selection of a strain exhibiting stable resistance to arteether. Exp Parasitol 2006; 114:129-132.

4. Bloland PB. A Contrarian view of malaria therapy policy in Africa. Am J Trop Med Hyg 2003; 68(2):125-126.

5. World Health Organization. Guidelines for the Treatment of malaria (1st ed) World Malaria Report WHO/HTM/MAL/2006.1108.WHO, Geneva, 2006.

6. Nosten F, White NJ. Artemisinin-based combination treatment of falciparum malaria. Amer J Trop Med Hyg 2007; 77(6):181-192.

7. Chukwuebuka EU, Franklin CK, Emmanuel MU, Salome AC, Joy R, Anthony AA. Recent advances in particulate anti-malarial drug delivery systems: A review. Int J Drug Dev 2013;5(1) in press.

8. Semete B, Kalombo L, Katata L, Swai H. Nano-drug Delivery Systems: Advances in TB, HIV and Malaria Treatment. Smart Biomol Med 2010; 15-52.

9. Ogbonna A, Uneke C. Artemisinin-based Combination therapy for uncomplicated malaria in Sub-Saharan Africa: the efficacy, safety, resistance and policy implementation Abuja 2000. Trans Roy Soc Trop Med Hyg 2008; 102(7):621-627.

10. Lindegardh N, Hampithakong W, Kamanikom B, Singhasivanon P, Socheat D, Yi P et al. Major pitfalls in the measurement of artemisinin derivatives in plasma in clinical studies. J Chromatogr B 2008; (876):54-60.

11. Thanh NV, Cowman AF, Hipgrave D, Kim TB, Phuc BQ, Cong LD, et al. Assessment of susceptibility of Plasmodium falciparum to Chloroquine, Quinine, Mefloquine, Sulphadoxine-Pyrimethamine and Artemisinin in Southern Vietnam. Trans Royal Soc Trop Med Hyg 2009; 95:513-517.

12. Attama AA, Momoh MA and Builders PF. Lipid nanoparticulate drug delivery systems: a revolution in dosage form design and development, recent advances in novel drug carrier systems, Sezer AD (Ed.), InTech, DOI: 10.5772/50486,

13. Fouad EA, El-badry M, Mahrous GM, Alsarra AI, Alashbban Z, and Alanazi FK. In vitro investigation for embedding dextromethorphan in lipids using spray drying. Digest J Nano Bio 2011; 6(3):1129-1139.

14. Umeyor EC, Kenechukwu FC, Ogbonna JD, Chime SA and Attama AA. Preparation of novel solid lipid microparticles loaded with gentamicin and its evaluation in vitro and in vivo. J. Microencapsul 2012; 1- 12. DOI: 10.3109/02652048.2011.651495.

15. Chime SA, Attama AA, Builders PF and Onunkwo GC. Sustained release diclofenac potassium-loaded solid lipid microparticle, based on solidified reverse micellar solution (SRMS): In vitro and in vivo evaluation. J Microencapsul 2013;30(4):335-345.

16. Chime SA, Onyishi VI, Brown SA, Attama AA, Idogwu EC, Onunkwo GC. Diclofenac potassium–loaded dika fat solid lipid microparticles: In vitro and in vivo characterisation. Bio Med Rx 2013; 1(3):227-234.

17. Joshi NH, Shah N. Review of lipids in pharmaceutical drug delivery system, part I, Amer Pharm Rev Russel Public 2008.

18. Pouton CW. Lipid formulations for oral administration of drugs: non emulsifying, self – emulsifying and self micro emulsifying drug delivery systems. Eur J Pharm Sci 2000; 11:93-98.

19. Rawat M, Saraf S. Liposphere: emerging carries in delivery of proteins and peptides, Int. Journal of Pharm. Sci. and Nanotechnology 2008; 1(3):207-214.

20. Masters DB, Domb AJ. Lipospheres local anesthetic timed release for perineural site application. Pharm Res 1998; 15:1038- 1045.

21. Khopade A.J., Jain NK. Long circulating lipospheres targeted to inflamed tissue, Pharmizie 1997; 52:165-166.

22. Domb AJ, Marlinsky A, Maniar M, Teomim L. Insect repellant formulations of N.N diethyl- m- toluamide (DEET) in a liposphere system: Efficiency and skin uptake. J Am Mosqu control Assoc 1995;11: 29- 34.

23. Amselem S, Alving CR, Domb AJ. Polymeric biodegradable lipospheres as vaccine delivery system. Polym Adv Tech 1992; 3:351-357.

24. Domb AJ, Maniar M. Liposphere for controlled delivery of substances. European Patent EP0502119, 1996.

25. Domb AJ, Bergelson L, Amselem S. Lipospheres for controlled delivery of substances. In Benita S. (ed), microencapsulation: method and industrial applications, Marcel Dekker Inc. NY 1996: 337- 410.

26. Chime SA, Onyishi VI and Onunkwo G.C. In vitro properties of solid lipid microparticles (SLMS) loaded with methanolic extract of Garcinia kola (heckel) seed. Inno J Ayurv Sci 2013; 1(1):16-20.

27. Chime SA, Onyishi VI, Obitte NC, Onunkwo GC, Odo GI. Sustained release artemether-loaded solid lipid microparticles, based on solidified reverse micellar solution (SRMS) Inno J Sci 2013; 1(2):1-7.

28. Attama AA, Igbonekwu CN. In vitro properties of surface-modified solid lipid microspheres containing an antimalarial drug: Halofantrine. Asian Pac J Trop Med 2011; 4(4): 253-258.

29. Higuchi T. Mechanism of sustained-action medication: Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci 1963; 52:1145-1149.

30. Ritger PL and Peppas NA. A simple equation for description of solute release 1. Fickian and non- Fickian release from non swellable device in the form of slabs, spheres, cylinders and discs. J Cont Rel 1987; 5:23-36.

31. Chime SA, Onunkwo GC and Onyishi IV. Kinetics and Mechanisms of Drug Release from Swellable and Non Swellable Matrices: A Review. Res J Pharm Bio Chem Sc 2013; 4 (2): 97-103.
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