Development of Cathelicidin in Liposome Carrier Using Thin Layer Hydration Method

Abstract

Objective: The purpose of this study was to produce an optimum liposome formulation and to study the effect of formulation parameter such as phospholipid amount and hydration time on characteristics of liposome containing Cathelichidin. Methods: Liposomes were prepared using a thin layer hydration method. Characterization of liposomes included organoleptic, PSA (Particle Size Analyzer) and zeta potential, entrapment efficiency, morphology by TEM (Transmission Electron Microscopy), the chemical interaction by FTIR (Fourier Transform Infrared Spectroscopy), and the stability by using Freeze-Thaw method. Results: The result of the organoleptic test showed that the liposome were in the form of milky white dispersion, odorless, and without sedimentation. Optimum formula was obtained by making variations of soy oil: cholesterol 10: 0 (F1), 9: 1 (F2), 8: 2 (F3), 7: 3 (F4), and variations in sonication time (10 and 30 min). Based on the results, it was found that the optimum sonication time was 30 min. F2 and F3 were chosen as the most optimum formulas with particle sizes of 190.3±6.8 nm and 212.9±4.4 nm; polydispersity index of 0.192±0.023 and 0.137±0.022, and zeta potential as much as-38.8±0.6 mV and-34.8±2.0 mV. To the optimum formula, cathelicidin was loaded with hydration time varies of 100 and 120 min. Longer hydration time resulted in smaller particle size and higher entrapment efficiency either for F2 or F3. TEM characterization revealed a spherical shape of liposomes from the optimum formula. The results of FTIR characterization did not show any interaction between the phospholipids of liposomes with cathelicidin. The data from the stability test showed good stability for F2 and F3 with a hydration time of 120 min, indicated by a p-value>0.05, which indicated that there was no significant change in the zeta potential for three Freeze-Thaw cycles. Conclusion: Formula of liposom using a variation of soy oil: cholesterol 9:1 and 8:2 with hydration time of 120 min revealed the best result with good stability for three Freeze-Thaw cycles.

Optimization and Characterization of Quercetin Vitamin C Nano-Phytosome Formulation

“…Cholesterol as a constituent of the hydrophobic walls of nano-phytosomes provides strength and rigidity to nano-phytosome particles/globules and increases particle stability so they are not easily damaged [16]. However, excessive addition of cholesterol in the formulation can affect the permeability of phytosome molecules and increase the size of their globules [26].…”

“…Meanwhile, in the nano-phytosome spectrum, the typical peak of quercetin is still visible, but there are additional of 2 new peaks in the range of 2840-3000 cm -1 (2924.13; 2853.73) region, which indicates the presence of C-H stretching, originating from soy lecithin and cholesterol [26]. There is also a slight shift in the carbonyl bond and carbon double bond markers (1741.75; 1646.27), which indicates that vitamin C is also involved in the nano-phytosome.…”

Pengembangan Peptida Antimikroba Sintesis (KR-12) dalam Sistem Vesikular Liposom

“…Meskipun KR-12 dapat mempertahankan aksi antibakteri, tetapi kerentanan Peptida Antimikroba terhadap degradasi enzimatik dan protease tidak dapat diubah pada kondisi fisiologis dan membutuhkan matriks perlindungan untuk mendapatkan pengobatan yang efisien. Liposom menawarkan kemungkinan dalam mengenkapsulasi dan melindungi peptida dari degradasi enzimatik dan protease (1) (11). Berdasarkan permasalahan di atas, peneliti tertarik untuk mengembangkan penghantaran obat dengan sistem vesikular liposom berbahan aktif peptida antimikroba sintesis KR-12.…”

“…Pada penelitian Blasi-Romero et al, (2023), mengatakan bahwa peptida antimikroba yang di formulasikan ke dalam bentuk nanoselulosa dan peptida antimikroba yang di formulasikan ke dalam bentuk nanopartikel polimer menunjukkan hasil yang lebih stabil dan efektivitas yang lebih besar (1) (12). Pemanfaatan nanoteknologi sebagai strategi yang tepat untuk meminimalkan keterbatasan karakteristik yang tidak diinginkan pada Peptida Antimikroba telah dilaporkan bahwa nanostruktur khususnya pada enkapsulasi liposom dapat menunjukkan toksisitas yang rendah, penurunan degradasi dan peningkatan efisiensi pengobatan (11).…”