Kajian Formulasi dan Bioavailabilitas Penghantaran Insulin Liposom Oral
Abstract
ABSTRACT: Insulin is a protein hormone used for diabetes mellitus' therapy. The problem of administering the insulin through the oral route is due to a large molecular size of the insulin because insulin and it will be degraded by enzymes in the gastrointestinal tract. The object of this study was to examine the formula and the release of liposomal system and to determine the bioavailability of insulin in the oral route with the liposomal delivery system. The study was carried out using a systematic literature review method by collecting data in the form of scientific research that had been conducted and published. The result of this study revealed that a good insulin liposome formulation can be achieved by using phosphatidylcholine and cholesterol in the ratio (7:3). The release of insulin into the systemic pathway occured when the lipids in liposomes were completely inserted in the biological membrane, then the insulin moved to the extracellular space. The bioavailability of oral liposome insulin was not better when compared with insulin administration through the subcutaneous route because the Cmax and Tmax values produced by subcutaneous administration were, respectively, higher with values of 82.1 ± 3μIU/ml and 1.0 ± 0.0/h compared to the administration of insulin through the oral route was 35.4 ± 2.8μIU/ml and 8.0 ± 0.0/h.
Keywords: Insulin, Oral, Liposomes, Formulation, Bioavailability.
ABSTRAK: Insulin merupakan hormon protein yang digunakan untuk terapi penyakit diabetes melitus. Permasalahan pemberian insulin melalui rute oral dikarenakan insulin memiliki ukuran molekul yang besar serta insulin akan terdegradasi oleh enzim pada jalur gastrointestinal. Tujuan dari penelitian ini untuk mengkaji formula dan pelepasan sistem liposom serta mengetahui bioavailabilitas insulin pada rute oral dengan sistem penghantaran liposom. Penyusunan dilakukan dengan metode systematic literature review yang dilakukan dengan pengumpulan data pustaka berupa penelitian ilmiah yang sudah dilakukan dan dipublikasikan. Hasil dari kajian ini adalah formulasi liposom insulin yang yang baik dapat dicapai dengan penggunaan fosfatidilkolin dan kolesterol pada ratio (7:3). Pelepasan insulin menuju jalur sistemik terjadi ketika lipid pada liposom tersisipkan dengan sempurna pada membran biologis kemudian insulin berpindah ke ruang ektraseluler. Bioavabilitas insulin liposom oral tidak lebih baik jika dibandingkan dengan pemerian insulin melalui rute subkutan karena nilai Cmax dan Tmax berturut-turut yang dihasilkan pada pemberian subkutan lebih besar dengan nilai 82,1 ± 3μIU/ml dan 1,0 ± 0.0/h dibandingkan dengan pemerian melalui rute oral adalah 35,4 ± 2,8μIU/ml dan 8,0 ± 0,0/h.
Kata Kunci: Insulin, Oral, Liposom, Formulasi, Bioavailabilitas
Keywords
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DOI: http://dx.doi.org/10.29313/.v0i0.29234
