Kajian Metode Bottom-Up pada Pembuatan Nanokristal Obat Antidiabetika Oral BCS Kelas II

Santy Juliarti (Prodi Farmasi, Fakultas Farmasi dan Sains, Universitas Islam Bandung, Indonesia)
Fitrianti Darusman (Prodi Farmasi, Fakultas Farmasi dan Sains, Universitas Islam Bandung, Indonesia)
Hanifa Rahma (Prodi Farmasi, Fakultas Farmasi dan Sains, Universitas Islam Bandung, Indonesia)

Bandung Conference Series: Pharmacy
527 - 534

Abstract. Oral antidiabetic drugs included in the Biopharmaceutics Classification System (BCS) class II have high permeability but low solubility, thus limiting the dissolution rate and oral bioavailability. One approach developed to overcome this problem is nanocrystal technology using the bottom-up method. This study aims to assess the effectiveness of the bottom-up method in the manufacture of nanocrystals of oral antidiabetic drugs BCS class II in improving physicochemical characteristics. This study was conducted using a literature review method of scientific articles obtained through Google Scholar, ResearchGate, and other scientific sources. Data were analyzed descriptively and presented in narrative form. The results of the study indicate that the bottom-up method is able to produce nanocrystals measuring less than 1000 nm, thereby increasing the specific surface area of ​​the particles, which has an impact on increasing solubility, dissolution rate, and potentially increasing oral bioavailability. The sonication-precipitation method is the most widely used method because it produces smaller particle sizes, a more homogeneous size distribution, and better stability. The success of this method is influenced by the selection of solvents, antisolvents, stabilizers, and process parameters. Thus, the bottom-up method is an effective approach in the development of BCS class II oral antidiabetic drug nanocrystals. Abstract. Oral antidiabetic drugs included in the Biopharmaceutics Classification System (BCS) class II have high permeability but low solubility, thus limiting the dissolution rate and oral bioavailability. One approach developed to overcome this problem is nanocrystal technology using the bottom-up method. This study aims to assess the effectiveness of the bottom-up method in the manufacture of nanocrystals of oral antidiabetic drugs BCS class II in improving physicochemical characteristics. This study was conducted using a literature review method of scientific articles obtained through Google Scholar, ResearchGate, and other scientific sources. Data were analyzed descriptively and presented in narrative form. The results of the study indicate that the bottom-up method is able to produce nanocrystals measuring less than 1000 nm, thereby increasing the specific surface area of ​​the particles, which has an impact on increasing solubility, dissolution rate, and potentially increasing oral bioavailability. The sonication-precipitation method is the most widely used method because it produces smaller particle sizes, a more homogeneous size distribution, and better stability. The success of this method is influenced by the selection of solvents, antisolvents, stabilizers, and process parameters. Thus, the bottom-up method is an effective approach in the development of BCS class II oral antidiabetic drug nanocrystals. Abstrak. Obat antidiabetika oral yang termasuk dalam Biopharmaceutics Classification System (BCS) kelas II yang memiliki permeabilitas tinggi, namun kelarutan rendah sehingga membatasi laju disolusi dan bioavailabilitas oral. Salah satu pendekatan yang dikembangkan untuk mengatasi permasalahan tersebut adalah teknologi nanokristal menggunakan metode bottom-up. Penelitian ini bertujuan untuk mengkaji efektivitas metode bottom-up dalam pembuatan nanokristal obat antidiabetika oral BCS kelas II terhadap peningkatan karakteristik fisikokimia. Penelitian ini dilakukan menggunakan metode literature review terhadap artikel ilmiah yang diperoleh melalui Google Scholar, ResearchGate, serta sumber ilmiah lainnya. Data dianalisis secara deskriptif dan disajikan dalam bentuk naratif. Hasil kajian menunjukkan bahwa metode bottom-up mampu menghasilkan nanokristal berukuran kurang dari 1000 nm sehingga mampu meningkatkan luas permukaan spesifik partikel, yang berdampak pada peningkatan kelarutan, laju disolusi, dan berpotensi meningkatkan bioavailabilitas oral. Metode sonikasi–presipitasi merupakan metode yang paling banyak digunakan karena menghasilkan ukuran partikel yang lebih kecil, distribusi ukuran yang lebih homogen, serta stabilitas yang lebih baik. Keberhasilan metode ini dipengaruhi oleh pemilihan pelarut, antisolvent, stabilizer, dan parameter proses. Dengan demikian, metode bottom-up merupakan pendekatan yang efektif dalam pengembangan nanokristal obat antidiabetika oral BCS kelas II.