METODE PENAMBAHAN SURFAKTAN SEBAGAI SUBSTRAT PG-P UNTUK MENINGKATKAN KELARUTAN OBAT LIPOFILIK : ARTICLE REVIEW

Amira Nur Hasanah, Taofik Rusdiana

Abstract


Saat ini, pengembangan obat berkembang cepat dan terus dilakukan. Salah satu permasalahan formulasi yang mempengaruhi efektivitas obat adalah kelarutan, terutama pada obat dengan kelarutan rendah. Obat-obat yang termasuk BCS kelas II mempunyai sifat permeabilitas tinggi dengan kelarutan rendah karena termasuk obat lipofilik. Metode yang digunakan untuk meningkatkan kelarutan adalah penambahan surfaktan sebagai substrat p-glikoprotein. Tujuan formulasi tersebut adalah mendapatkan bioavailabilitas untuk mencapai efek terapetik. Penambahan surfaktan sudah dibuat dalam berbagai bentuk sediaan, seperti nanokristal, granul, mikroemulsi, dan lain-lain. Hasil dari berbagai penambahan surfaktan dan bentuk sediaan tersebut berfungsi sebagai substrat p-glikoprotein sehingga kelarutan obat lipofilik meningkat dan bioavailabilitasnya menjadi lebih baik.

 

Kata Kunci: surfaktan, BCS kelas II, kelarutan.


References


Agrawal, S., Giri, T. K., Tripathi, D. K., Ajazuddin., and Alexander, A. 2012. A Review on Novel Therapeutic Strategies for the Enhancement of Solubility for Hydrophobic Drugs through Lipid and Surfactant Based Self Micro Emulsifying Drug Delivery System: A Novel Approach. American Journal of Drug Discovery and Development. 2: 143-183.

Ajazuddin and Saraf, S. 2010. Applications of Novel Drug Delivery System for Herbal Formulations. Fitoterapia. 81: 680-689.

Akhter, Md. H., Mohan, G., Hedaitullah, Md., Iqbal, Md. K. 2014. Lipid Based Drug Delivery System: Classification, Drug Transport Across Enterocyte, Role of Lipid Chain Length in Suppression of Body Fat Accumulation. International Journal of Pharmacy. 4(2): 98-108.

Aungst, B. J. 1993. Novel Formulation Strategies for Improving Oral Bioavailability of Drugs with Poor Membrane Permeation or Pre-systemic Metabolism. J Pharm Sci. 82: 979-987.

Bandarkar, S. F. and Ibrahim, S. K. 2011. Lyophilized Gliclazidepoloxamer, Solid Dispersions for Enhancement of In Vitro Dissolution and In Vivo Bioavailability. Int J Pharm Pharm Sci. 3: 122-127.

Chen, M.L. 2008. Lipid Excipients and Delivery Systems for Pharmaceutical Development: a Regulatory Perspective. Adv Drug Deliv Rev. 60(6): 768-77.

Chen, Y., H. Zhang, H. W., and Yang, K. 2011. Effects of Dietary Addition of Non-Ionic Surfactants on Ruminal Metabolism and Nutrient Digestion of Chinese Merino Sheep. Asian J. Anim. Vet. Adv.6: 688-696.

Cherniakov, I., Domb, A. J., and Hoffman, A. 2015. Selfnano-emulsifying Drug Delivery Systems: an Update of the Biopharmaceutical Aspects. Expert Opinion on Drug Delivery. 12(7): 1121-1133.

Choi, Y. K., Poudel, B. K., Marasini, N., et al. 2012. Enhanced Solubility and Oral Bioavailability of Itraconazole by Combining Membrane Emulsification and Spray Drying Technique. International Journal of Pharmaceutics. 434(1-2): 264–271.

Ferte, J. 2000. Analysis of Tangled Relationships between P-glycoprotein Mediated Multidrug Resistance and the Lipid Phase of the Cell Membrane. Eur. J. Biochem. 267(2): 277-294.

Gaucher, G., Satturwar, P., Jones, M.C., A. Furtos, and Leroux, J.-C. 2010. Polymeric Micelles for Oral Drug Delivery. European Journal of Pharmaceutics and Biopharmaceutics. 76(2): 147–158.

Giri, T.K., H. Badwaik, Alexander, A., and Tripathi, D. K. 2010. Solubility Enhancement of Ibuprofen in the Presence of Hydrophilic Polymer and Surfactant. Int. J. Applied Biol. Pharm. Technol. 1: 793-800.

Hodaei, D., Baradaran, B., Valizadeh, H., and Milani, P.Z. 2015. Effects of Polyethylene Glycols on Intestinal Efflux Pump Expression and Activity in Caco-2 Cells. Brazilian Journal of Pharmaceutical Sciences. 51(3).

Kalepu, S., Manthina, M., and Padavala, V. 2013. Oral Lipid-based Drug Delivery Systems – an Overview. Acta Pharmaceutica Sinica B. 3(6): 361-372.

Kommuru, T. R., Gurley, B., Khan, M.A., Reddy, I.K. 2001. Self-emulsifying Drug Delivery Systems (SEDDS) of Coenzyme Q10: Formulation Development and Bioavailability Assessment. Int. J. Pharm. 212: 233-246.

Lachman, L., Lieberman, H., and Kanig, J. L. 1986. The Theory And Practise of Industrial Pharmacy. 3rd edition. Lea & Febiger.

Lipinski, C. A. 2000. Drug-like Properties and the Causes of Poor Solubility and Poor Permeability. Journal of Pharmacological and Toxicological Methods. 44(1): 235–249.

Mohd, A. B. and Vemula, S. K. 2016. Formulation and Pharmacokinetics of Vitamin E TPGS Melt Dispersion Granules: An Approach to Improve Oral Delivery of Flurbiprofen. J Bioequiv. Availab 8: 089-94. doi:10.4172/jbb.1000274.

Mohsin, K., Long, M. A., and Pouton, C. W. 2009. Design of Lipid-based Formulations for Oral Administration of Poorly Water-soluble Drugs: Precipitation of Drug After Dispersion of Formulations in Aqueous Solution. J. Pharm. Sci. 98: 3582-3595.

Noudeh, G. D., Khazaeli, P., and Rahmani, P. 2008. Study of the Effects of Polyethylene Glycol Sorbitan Esters Surfactants Group on Biological Membranes. Int. J. Pharmocol. 4: 27-33.

Peltonen, L., and Strachan, C. 2015. Understanding Critical Quality Attributes for Nanocrystals from Preparation to Delivery. Molecules. 20 : 22286-223000. Published online at doi:10.3390/molecules201219851.

Pouton, C. W. 2006. Formulation of Poorly Water-soluble Drugs for Oral Administration: Physicochemical and Physiological Issues and the Lipid Formulation Classification System. Eur J Pharm Sci. 29: 278–87.

Savjani, K. T., Gajjar, A. K., & Savjani, J. K. 2012. Drug Solubility: Importance and Enhancement Techniques. ISRN Pharmaceutics 2012. 195727. http://doi.org/10.5402/2012/195727.

Srivalli, K. M. R., and Mishra, B. 2016. Improved Aqueous Solubility and Antihypercholesterolemic Activity of Ezetimibe on Formulating with Hydroxypropyl-β-Cyclodextrin and Hydrophilic Auxiliary Substances. AAPS Pharm SciTech. 17(2): 272-283.

Swarbrick J. 2007. Encyclopedia of Pharmaceutical Technology. 3rd edition. New York: Informa Health Care.

Tejeswari, N., Harini, C. V, Hyndavi, N., Jyotsna, T., Gowri, Y., and Raju, Y.P. 2014. Lipid Based Drug Delivery System for Enhancing Oral Bioavailability – A Contemporary Review. Journal of Global Trends in Pharmaceutical Science. 5(4): 2074-2082.

Thiebaut, F., Tsuruo, T., Hamada, H., et al. 1987. Cellular Localization of the Multidrugresistance Gene Product P-glycoprotein in Normal Human Tissues. Proc Natl Acad Sci USA. 84(21): 7735-8.

Todeschini, V., Sangoi, M. S., Goelzer, G. K., Machado, J. C., Paim, C. S., Araujo, B. V., and Volpato, N. M. 2016. Dissolution Method for Delapril and Manidipine Combination Tablets Based on an Absorption Profile of Manidipine. Journal of Pharmaceutical Analysis. 6(1) : 49-55.

Varshosaz, J., Ziaei, V., Minaiyan, M., Najafabadi, A. J., and Tabatabaei, L. S. 2018. Enhance Solubility, Oral Bioavailability, and Anti-Osteoporotic Effects of Raloxifene HCl in Ovariectomized Rats by Igepal CO-890 Nanomicelles. Journal Pharmaceutical Development and Technology. Published online at https://doi.org/10.1080/10837450.2018.1428815.

Xu, W., Ling, P., and Zhang, T. 2013. Polymeric Micelles, a Promising Drug Delivery System to Enhance Bioavailability of Poorly Water-Soluble Drugs. Journal of Drug Delivery. vol. 2013. Article ID 340315, 15pages,. https://doi.org/10.1155/2013/340315.

Yi, T., Wan, J., Xu, H., and Yang, X. 2008. A New Solid Self-emulsifying Formulation Prepared by Spray-drying to Improve the Oral Bioavailability of Poorly Soluble drugs. Eur J Pharm Biopharm. 70: 439–444.

Yu, L.X. and Amidon, G. L. 1999. A Compartmental Absorption and Transit Model for Estimating Oral Drug Absorption. Int. J. Pharm. 186: 119-125.




DOI: https://doi.org/10.24198/jf.v16i2.17620

DOI (PDF (Bahasa Indonesia)): https://doi.org/10.24198/jf.v16i2.17620.g8700

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