Kajian Pengaruh Sistem Nanoemulsi terhadap Penghantaran Oral Agen Antihiperlipidemia

Ega Destiyani, Sani Ega Priani, Mentari Luthfika Dewi

Abstract


ABSTRACT: Hyperlipidemia is the main risk factor for coronary heart disease (CHD), stroke, pancreatitis, and atherosclerosis. Some oral antihyperlipidemic active substances are included in the Biopharmaceutical Classification System (BCS) class II drugs that are drugs with low solubility in water, resulting in low dissolution profile, bioavailability, and pharmacological effects. Nanoemulsion is a drug delivery system that can increase solubility and absorption of active substances in the gastrointestinal tract. This literature study aims to determine the effect of nanoemulsion development on dissolution, bioavailability, and pharmacological effects of active substances with antihyperlipidemic activity. It used a Systematic Literature Review (SLR) method covering some stages of design, search, download, selection, and determination of articles based on inclusion criteria. The study on antihyperlipidemic agents, namely simvastatin, raspberry ketone, atorvastatin, and ezetimibe showed that the nanoemulsion formula could increase dissolution indicated by the higher concentration of drug released within a certain time than suspension and tablets. The nanoemulsion formula could also increase the bioavailability of drugs characterized by higher Cp, Cmax, and AUC values compared to suspensions and tablets. The nanoemulsion formula could also increase the effectiveness of the drug characterized by a decrease in the levels of TC, TG, and an increase in HDL levels better than suspension and tablets.

Keywords: Systematic Literature Review (SLR), nanoemulsion, antihyperlipidemic agent

ABSTRAK: Hiperlipidemia merupakan faktor resiko utama penyebab penyakit jantung koroner (PJK), stroke, pankreatitis dan aterosklerosis. Diketahui beberapa zat aktif antihiperlipidemia oral termasuk dalam Biopharmaceutical Classification System (BCS) kelas II, yang merupakan obat-obatan dengan kelarutan yang rendah dalam air sehingga berdampak pada rendahnya profil disolusi, bioavailabilitas, dan efek farmakologi yang dihasilkan. Nanoemulsi adalah salah satu sistem penghantaran obat yang mampu meningkatkan kelarutan dan meningkatkan penyerapan zat aktif di saluran cerna. Studi literatur ini bertujuan untuk mengetahui pengaruh pengembangan nanoemulsi terhadap disolusi, bioavailabilitas, dan efek farmakologi dari zat aktif dengan aktivitas antihiperlipidemia. Metode penelitian yang digunakan adalah Systematic Literature Review (SLR) dengan beberapa tahapan diantaranya perancangan, pencarian, pengambilan, seleksi, dan penentuan artikel berdasarkan kriteria inkulsi. Hasil kajian yang dilakukan terhadap agen antihiperlipidemia yaitu simvastatin, rashberry keton, atorvastatin, dan ezetimibe menunjukan bahwa formula nanoemulsi mampu meningkatkan disolusi yang ditandai dengan kadar obat yang berhasil dilepaskan dalam waktu tertentu jauh lebih tinggi dibandingkan dengan suspensi dan tablet. Formula nanoemulsi juga mampu meningkatkan bioavailabilitas obat yang ditandai dengan nilai Cp, Cmax, dan AUC yang lebh tinggi dibandingkan dengan suspensi dan tablet. Formula nanoemulsi juga mampu meningkatkan efektivitas obat yang ditandai dengan penurunan kadar TC, TG dan peningkatan kadar HDL lebih baik dibandingkan dengan suspensi dan tablet.

Kata Kunci: Sytematic Literature Review (SLR), nanoemulsi, agen antihiperlipidemia


Keywords


Sytematic Literature Review (SLR), nanoemulsi, agen antihiperlipidemia

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References


Asmarani, C. F. Iis Wahyuningsih. (2015). Pengaruh Variasi Konsentrasi Tween 80 dan Sorbitol terhadap Aktivitas Antioksidan Minyak Zaitun (Oleum olivae) dalam Formulasi Nanoemulsi. Yogyakarta: Farmasains.

Azeem, A. et al. (2009). Nanoemulsion Components Screening and Selection a Technical Note. AAPS PharmSciTech. 10:68-76.

Bali, V., Ali, M., & Ali, J. (2010a). Novel nanoemulsion for minimizing variations in bioavailability of ezetimibe. Journal of Drug Targeting, 18(7), 506–519. https://doi.org/10.3109/10611860903548362

Bali, V., Ali, M., & Ali, J. (2010b). Study of surfactant combinations and development of a novel nanoemulsion for minimising variations in bioavailability of ezetimibe. Colloids and Surfaces B: Biointerfaces, 76(2), 410–420. https://doi.org/10.1016/j.colsurfb.2009.11.021

Bhatnagar D, Soran H, Durrington PN. Hypercholesterolemia and Its Management. British Medical Journal. 2008;337:503-508.

Chavhan, S. S., Petkar, K. C., & Sawant, K. K. (2013). Simvastatin nanoemulsion for improved oral delivery: Design, characterisation, in vitro and in vivo studies. Journal of Microencapsulation, 30(8), 771–779. https://doi.org/10.3109/02652048.2013.788085

Devarajan, V., Ravichandran, V. (2011). Nanoemulsion: as modified drug delivery tool. International Journal of Comprehensive Pharmacy.

Dipiro, J. T., Dipiro, C.V., Wells, B.G., & Scwinghammer, T.L. (2008). Pharmacoteraphy. Handbook Seventh Edition, USA: McGraw-Hill Company.

Ige, P. P., Bachhav, N. A., Mahajan, H. S., Nerkar, P. P., & Gattani, S. G. (2013). Atorvastatin-Loaded Oleic Acid Nanoglobules for Oral Administration: In Vitro Characterization and Biopharmaceutical Evaluation. Current Nanoscience, 9(2), 202–210. https://doi.org/10.2174/1573413711309020007

Kasim, E., Kurniawati, Y., Nurhidayat N. (2006). Pemanfaatan Isolat local Monascus Purpureus Untuk Menurunkan Kolesterol Darah Pada Tikus Putih Galur Sprague Dawley.

Kemken, J., Ziegler, A. & Muller, B. (1992). Influence of supersaturation on the pharmacodynamic effect of bupranolol after dermal administration using microemulsions as vehicle. Pharm Res, 9:554Y558.

Kreilgaard, M., MJB Kemme, J. B., Schoemaker, R. & Cohen, A. (2001). Influence of a microemulsion vehicle on cutaneous bioequivalence of a lipophilic model drug assessed by microdialysis and pharmacodynamics. Pharm Res. 18:593Y59.

Kobayashi, M., Kagawa, T., Narumi, K., Itagaki, S., Hirano, T., Iseki, K. (2008). Bicarbonate supplementation as a preventive way in statins-induced muscle damage. Journal of Pharmacy & Pharmaceutical Sciences 11, 1-8.

Neal, M. J., (2005). Medical Pharmacology at a Glance, Edisi Kelima, 46-47, Erlangga, Jakarta.

Priani, S. E., Halim, A. F., Fitrianingsih, S. P., & Syafnir, L. (2021). Uji Aktivitas Inhibitor Tirosinase Ekstrak Kulit Buah Cokelat (Theobroma cacao L.) dan Formulasinya dalam Bentuk Sediaan Nanoemulsi. Jurnal Sains Farmasi & Klinis, 8(1), 1. https://doi.org/10.25077/jsfk.8.1.1-8.2021

Shafiq, S. et al. (2007). Design and development of oral oil in water ramipril nanoemulsion formulation: in vitro and in vivo evaluation. J Biomed Nanotech, Volume 3, pp. 28-44.

Shakeel, F., Baboota, S., Ahuja, A., Ali, J dan Shafiq, S. 2008. Celecoxib nanoemulsion: skin permeation mechanism and bioavailability assessment. Journal of drug targeting, 16(10):733-740.

Singh, S., Virmani, T., & Kohli, K. (2020). Nanoemulsion System for Improvement of Raspberry Ketone Oral Bioavailability. Indo Global Journal of Pharmaceutical Sciences, 10(01), 33–42. https://doi.org/10.35652/igjps.2020.10105

Suyatna, F.D., (2008). Farmakologi dan Terapi, edisi kelima, 374-385. Jakarta: Departemen Farmakologi dan Terapeutik Fakultas Kedokteran UI.

World Health Organization (2017). Global Health Observatory Data: Raised Cholesterol. WHO. Geneva.

Nurmilla Ani, Kurniaty Nety, W Hilda Aprillia. (2021). Karakteristik Edible Film Berbahan Dasar Ekstrak Karagenan dari Alga Merah (Eucheuma Spinosum). Jurnal Riset Farmasi, 1(1), 24-32.




DOI: http://dx.doi.org/10.29313/.v0i0.28944

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