Pengembangan Sistem Nanostructured Lipid Carriers (NLC) Meloxicam dengan Lipid Monostearin dan Miglyol 808 Menggunakan Metode Emulsifikasi
The aim this study was to determine the effect of Monostearin and Miglyol 808 lipid ratio in NLC system formulation resulting in physicochemical characteristics, release rate, and penetration rate. The NLC making was done by using emulsification method. In the formulation of NLC meloxicam, 3 different lipid ratios were used, including ratios of 6:4, 7:3, 8:2. Meloxicam served as active ingredient, monostearin served as solid lipid, miglyol 808 served as a liquid lipid, and tween 80 was surfactant. NLC meloxicam physicochemical characteristics include tests of organoleptic, pH, viscosity, particle size, particle morphology and entrapment efficiency. NLC meloxicam belongs to semisolid preparations with pH value range of 5,72-5,87. Increasing viscosity of NLC system are cause by increase of solid lipid. The measurement results of particle size of three different lipid formulas indicated that the lipid particle size was <1000 nm. Test of NLC particle morphology by using Transmission Electron Microscopy (TEM) indicated the spherical particle shape (round). Entrapment efficiency test of all NLC-lipid compositions revealed quite high result (> 80%). The determination of release rate (flux) and penetration rate (flux) was conducted by using Franz diffusion cells with a cellophane membrane for the release and Wistar ratâ€™s skin membrane for the penetration. The release rate values of three NLC meloxicam formulas showed p value (sig) 0,005, while the penetration rate obtained p value (sig) 0,091.
Keywords: NLC, meloxicam, physicochemical characterization, release rate and penetration rate
2.Bertram, G., and Katzung, MD., 2009. Basic and Clinical Pharmacology, 11th Ed, United States: McGraw-Hill Companies Inc, pp 817-819.
3.Bhaskar, K., Anbu, J., Ravichandiran, V., Venkateswarlu, V., and Rao, Y.M., 2009. Lipid Nanoparticles for Transdermal Delivery of Flurbiprofen: Formulation, in vitro, ex vivo and in vivo Studies. BioMed Cent8: 254-258.
4.Christina, 2010. Pengaruh Mentol, Etanol, dan Propilen Glikol Terhadap Profil Penetrasi Perkutan Glukosamin Secara in Vitro Menggunakan Sel Difusi Franz. Skripsi, Universitas Indonesia, Indonesia.
5.Cirri, M., Bragagni, M., Mennini, P., 2012. Development of a New Delivery System Consisting â€œDrug-in Cyclodextrin-in Nanostructured Lipid Carriersâ€ for Ketoprofen Topical Delivery. Eur J of Pharm and Biopharm80(1): 46-53.
6.El-Megrab, N., El-Nahas, H., Gehan.,F., 2006. Formulation and Evaluation of Meloxicam Gels for Topical Administration. Egypt J of Pharm14: 3-4.
7.Godin, B., and Touitou, E., 2007. Transdermal Skin Delivery: Prediction for Human Fron in Vivo, Ex Vivo and Animals Model. Adv Drug Deliv Rev59: 1152-1161.
8.Han, F., Li, Sanming, Yin, Ran, Liu, Hongzhuo, Xu, Lu, 2008. Effect of Surfactants on the Formation and Characterization of a new type of
Colloidal Drug Delivery System Nanostructured Lipid Carriers.
Inter J of Pharm315: 210-216.
9.Han, F., Yin,R., Che, X., Yuan, J., Cui, Y., Yin, H., Li, S., 2008.
Nanostructured Lipid Carriers (NLC) Based Topical Gel of Flurbiprofen: Design, Characterization and in Vivo Evaluation.
Inter J of Pharm439: 349â€“357.
10.Hu, F.Q., Jiang, S.P., Du, Y.Z., Yuan, H., Zeng, S., 2006. Preparation and Characteristics of Monostearin Nanostructured Lipid Carriers. Inter J of Pharm314: 83â€“89.
11.Joshi, M., and Patravale, V., 2008. Nanostructured Lipid Carrier(NLC) Based Gel of Celeco xib. Inter J of Pharm346: 124â€“132.
12.Khurana, S., Jain, N.K., Bedi, P.M.S., 2013. Development and Characterization of a Novel Controlled Release Drug Delivery System Based on Nanostructured Lipid Carriers Gel for Meloxicam. Life Sci
13.Muller, A.Z., Schwarz, C., Menhert, W., 1998. Solid Lipid Nanoparticles (SLN) for Controlled Drug Delivery-Drug Release and Release Mechanism. J of Pharm and Biopharm 45: 149-155.
14.Muller, R.H., Mader, K., Gohla, S., 2002. Solid Lipid Nanoparticles for Controlled DrugDelivery a Review of the State of the Art. Eur J of
Pharm and Biopharm50: 161-177.
15.Muller, R.H., Radike, M., Wissing, S.A., 2007. Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carrier (NLC) in Cosmetic and Dematological Preparations. Adv Drug Deliv Rev1: 131
16.Pardeike, J., Hommos, A., Muller, R.H., 2009. Lipid Nanoparticles (SLN and NLCs) in Cosmetic and Pharmaceutical Dermal Product.
Inter J of Pharm336: 170-184.
17.Phatak, A., and Chaudhari, P., 2013. Development and Evaluation of Nanostructured Lipid Carrier (NLC) Based Topical Delivery of an Anti-inflamatory Drug. J of Pharm Res7(8): 677-685.
18.Rowe, R.C., Sheykey, J.C., Quinn, M., 2009. Handbook of
Pharmaceutical Excipient. 6th Ed. USA: Pharmaceutical Press.
19.Sinko, Patrick, 2011. PhysicalPharmacy and Pharmaceutical Science. 6th Ed. Cina: Lippincot Williams & Wilkins, pp 355-367, 469-473.
20.Sivaramakrishnan, R., Nakamura, C., Mehnert, W., Korting, H.C., Kramer, K.D., Schafer-Korting, M., 2004. Glucocorticoid Entrapment Into Lipid Carriers Characterisation by Parelectric Spectroscopy and
Influence on Dermal Uptake. J of Cont Rel97: 493â€“502.
21.Souto, E.B., and Muller, R.H., 2007. Lipid Nanoparticles (Solid lipid Nanoparticles and Nanostructured Lipid Carriers) for Cosmetic, Dermal, and Transdermal Applications. Drug and Pharm Sci166: 213-232.
22.Souto, E.B., Wisiing, S.A., Barbosa, C.M., Muller, R.H., 2004. Development of a Controlled Release Formulation Based on SLN and NLC for Topical Clotrimazole delivery. Inter J of Pharm278: 71-77.