Formulasi Self-Nanoemulsifiying Drug Delivery System (SNEDDS) Asam Mefenamat menggunakan VCO dengan Kombinasi Surfaktan Tween dan Span

Mefenamic acid is a non-steroidal anti-inflammatory drug (NSAID) which has analgesic, anti-inflammatory and antipyretic effects. Mefenamic acid works by inhibiting prostaglandin synthesis as an inflammatory mediator. Mefenamic acid has low drug solubility and a long process of dissolution in the body which greatly affects the speed of absorption and bioavailability of the drug. In this study, mefenamic acid nanoemulsion formulation was carried out through a Self-Nanoemulsifying Drug Delivery System (SNEDDS) delivery system. SNEDDS is a drug delivery method through isotropic oil extraction, surfactants, cosurfactans and drug that form oil in water (m/a) emulsions which when in contact with the water phase in the digestive tract wiil from a nanoemulsion that occurs spontaneously so that the drug dissolves with a particle size small so as to increase the effective surface area for absorption. The purpose of the study was to determine the ratio of surfactant and cosurfactant composition to the optimum formula of SNEDDS of mefenamic acid with VCO as an oil phase. The SNEDDS formula was obtained by mixing the surfactants tween 80 and span 80, cosurfactant PEG 400 and VCO as the oil phase using the characterization of determining the optimum formula, namely emulsion formation, transmittance and emulsification time. The composition of the optimum formula of SNEDDS of mefenamic acid is 1 mL VCO; 1 mL PEG 400; 6 mL tween 80; 1 mL span 80. Optimum formula showed clear emulsion results, with transmittance values of 89,04% and emulsification time under 1 minute. In this study produced the optimum formula SNEDDS the met the criteria based on droplet size parameters of 153,5 nm, potential zeta value of 8,2 mV and showed good stability.

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Validasi Penetapan Kadar Isolat Andrografolid dari Tanaman Sambiloto (Andrographis paniculata Nees) Menggunakan HPLC

Jurnal Sains Farmasi & Klinis ◽

10.29208/jsfk.2015.2.1.42 ◽

2015 ◽

Vol 2 (1) ◽

pp. 8 ◽

Cited By ~ 1

Author(s):

Yandi Syukri ◽

Agung Endro Nugroho ◽

Ronny Martien ◽

Endang Lukitaningsih

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Tween 80 ◽

Andrographis Paniculata ◽

Peg 400

Penelitian ini bertujuan untuk mengembangkan analisis kuantitatif untuk penentuan kadar isolat andrographolide dari tanaman sambiloto (Andrographis paniculata) dan pelarut yang berbeda untuk studi awal untuk pembuatan Self Nanoemulsifying Drug Delivery System (SNEDDS) menggunakan KCKT. Pemisahan menggunakan kolom Sunfire C18 dengan campuran isokratik metanol dan air dengan perbandingan 6: 4, v / v sebagai fase gerak. Metode untuk menentukan isolat andrographolide menunjukkan presisi yang memadai, dengan RSD lebih kecil dari 1%. Akurasi dianalisis dengan menambahkan andrografolid standar, dan didapatkan nilai perolehan kembali yang baik untuk semua konsentrasi yang digunakan. Metode HPLC yang dikembangkan dalam penelitian ini menunjukkan spesifisitas dan selektivitas dengan linearitas dalam rentang kerja dan presisi dan akurasi yang baik, sehingga sangat cocok untuk menentukan kandungan isolat andrografolida. Dibandingkan dengan standar, kemurnian isolat andrografolida adalah 95,74 ± 0,29%. Penelitian awal untuk menentukan kelarutan tertinggi isolat andrographolid adalah dalam fasa minyak Capryol-90 1,226 ± 0,009 mg mL-1, surfaktan tween 80 2,965 ± 0.014 mg mL-1 dan co-surfaktan PEG 400 6,074 ± 0,101 mg mL-1. Dapat disimpulkan, metode ini cocok digunakan untuk penentuan kelarutan dari isolat andrographolide untuk pembuatan SNEDDS.

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Characterization and Optimization of Capryol-90, Polysorbate-80, And Peg-400 Proportion in Mefenamic Acid Self Nanoemulsifying Drug Delivery System (SNEDDS) With Simplex-Lattice-Design

Science & Technology Indonesia ◽

10.26554/sti.2018.3.4.164-172 ◽

2018 ◽

Vol 3 (4) ◽

pp. 164

Author(s):

Mardiyanto Mardiyanto ◽

Najma Annuria Fithri ◽

Martina Tandry

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Mefenamic Acid ◽

Polysorbate 80 ◽

Lattice Design ◽

Peg 400 ◽

Simplex Lattice Design ◽

Simplex Lattice ◽

Optimal Formula

Mefenamic acid as pain relief drug belongs to the biopharmaceutics classification system (BCS) class II which is practically insoluble in water causing extremely low dissolution in gastrointestinal tract. The self nanoemulsifying drug delivery system (SNEDDS) is a new innovation pharmaceutical dosage form that has effectively known to increase solubilization of hydrophobic drug in polar solvent. In this study the capryol-90 was selected as oil phase in SNEDDS as it showed maximal solubility of mefenamic acid (20 mg/mL). Combination of polysorbate-80 and PEG-400 as a generally regarded as safe (GRAS) excipient were used as surfactant and co-surfactant in SNEDDS due to its high HLB property that can increase mefenamic acid solubility in water. The ternary phase diagram of capryol-90, polysorbate-80, and PEG-400 was constructed in advance to obtain the component concentration of spontaneous nanoemulsion region. Model simplex-lattice-design cooperated in Design-Expert®10 was used to define SNEDDS mefenamic acid formula. Optimized mefenamic acid SNEDDS formula consisted of 20% capryol-90, 31.62% polysorbate-80, and 48.38% PEG-400. Characterization study of Optimized mefenamic acid SNEDDS formula showed improvement of drug content (102.820 ± 4.950)%, emulsification time (421.015 ± 1.290) second, and viscosity (0.927 ± 0.017) mm2/s 30oC. One way ANOVA statistical analysis result of optimal formula SNEDDS (105.210 ± 4.425)% of drug content, commercial generic caplet (0.917 ± 0.094)%, and mefenamic acid powder capsule (10.446 ± 0,333)% gave significant value (sig*) below than 0.05. Optimal formula proved that SNEDDS can significantly increase mefenamic acid dissolution of pH 7.4 (ileum fluid). The optimal formula of mefenamic acid SNEDDS successfully formed an uniformity droplet size (PDI 0.18) with mean size 241.9 nm and the surface charge has a value of -16.5 mV respectively.

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Formulation Studies of Solid Self-Emulsifying Drug Delivery System of Ivermectin

Folia Medica ◽

10.2478/folmed-2018-0024 ◽

2018 ◽

Vol 60 (4) ◽

pp. 580-593

Author(s):

Vipul P. Patel ◽

Hardik A. Lakkad ◽

Kalpesh Chhotalal Ashara

Keyword(s):

Drug Delivery ◽

Differential Scanning Calorimetry ◽

Fourier Transform ◽

Drug Delivery System ◽

Delivery System ◽

Oral Bioavailability ◽

Tween 80 ◽

Scanning Calorimetry ◽

Span 80

Abstract Background: The suggested dose of ivermectin is 300 μG/kg/day for onchocerciasis but it has low water solubility and poor oral bioavailability. Aim: To prepare and evaluate a solid lipid-based self-emulsifying drug delivery system of ivermectin. Materials and methods: Based on supersaturated solubility study, oil, surfactant, and co-surfactant were selected. On the basis of ternary phase diagrams and simplex-lattice design, self-emulsifying, drug delivery formulations had been developed and optimized. Ivermectin-excipients compatibility studies were performed using differential scanning calorimetry and Fourier transform infrared spectroscopy. Solid self-emulsifying drug delivery formulation was formulated from the optimized batch by surface assimilation method and filled into hard gelatin capsules. In vitro release rate and in vivo pharmacokinetic parameters of ivermectin from the capsules were determined. Two-tailed paired t-test/Dunnett multiple comparison tests were performed for in vivo pharmacokinetic parameter at 95 % of confidence level. Results: Soybeans oil, tween 80, and span 80 were selected as oil, surfactant, and co-surfactant respectively. The ternary diagrams were shown the maximum area for emulsion in 1:2 surfactant/co-surfactant ratio. The optimized batch had found with 30 mg ivermectin, 6.17 g soybeans oil, 0.30 g tween 80, and 3.50 g span 80. All differential scanning calorimetry and Fourier transform infrared characteristic peaks of the optimized formulation were identical with that of pure ivermectin. The area under the curve of ivermectin from the capsule was about two-fold higher than that of ivermectin suspension. Conclusions: Solid self-emulsifying drug delivery system was an effective oral solid dosage form to improve the oral bioavailability of ivermectin.

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Penggunaan D-Optimal Mixture Design untuk Optimasi dan Formulasi Self-Nano Emulsifying Drug Delivery System (SNEEDS) Asam Mefenamat

Jurnal Sains Farmasi & Klinis ◽

10.25077/jsfk.7.3.180-187.2020 ◽

2020 ◽

Vol 7 (3) ◽

pp. 180

Author(s):

Yandi Syukri ◽

Bambang Hernawan Nugroho ◽

Istanti Istanti

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Tween 80 ◽

Mixture Design ◽

Peg 400

Penelitian ini bertujuan untuk melakukan optimasi formulasi asam mefenamat yang sukar larut dalam air dalam bentuk sediaan Self-Nano Emulsifying Drug Delivery System (SNEDDS) menggunakan D-optimal mixture design. Skrining awal dilakukan untuk menentukan fase minyak, surfaktan dan ko-surfaktan yang akan digunakan untuk pembuatan diagram fase terner. D-optimal mixture design digunakan untuk mengoptimasi SNEDDS asam mefenamat dengan memilih komposisi SNEDDS sebagai faktor independent dan karakterisasi SNEDDS sebagai respons. Karakterisasi SNEDDS pada formula optimal meliputi transmitan, ukuran partikel, polidispersity index (PDI) dan zeta potensial. Asam oleat, Tween 80, dan polietilenglikol (PEG) 400 merupakan fase minyak, surfaktan, dan ko-surfaktan yang terpilih karena memiliki kemampuan paling tinggi dalam melarutkan asam mefenamat. Hasil optimasi menunjukkan bahwa formula optimal diperoleh pada komposisi 10% asam oleat, 80% Tween 80 dan 10% PEG 400. SNEDDS asam mefenamat tersebut menghasilkan nanoemulsi dengan transmitan 88,5%, ukuran partikel 190,03 ± 1,18 nm, PDI 0,469 ± 0,03, dan zeta potensial -44,1 ± 1,69 mV. Studi ini menyimpulkan bahwa D-optimal mixture design dapat digunakan untuk mengoptimasi dan formulasi SNEDDS asam mefenamat yang sukar larut dalam air.

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Preparation, Characterization and In Vitro Release Study of Microcapsule Simvastatin Using Biodegradable Polymeric Blend of Poly(L-Lactic Acid) and Poly(ɛ-Caprolactone) with Double Emulsifier

Materials Science Forum ◽

10.4028/www.scientific.net/msf.977.178 ◽

2020 ◽

Vol 977 ◽

pp. 178-183

Author(s):

Findi Citra Kusumasari ◽

Lukmanul Hakim Samada ◽

Emil Budianto

Keyword(s):

Adverse Effect ◽

Drug Delivery ◽

Lactic Acid ◽

Drug Release ◽

Drug Delivery System ◽

Delivery System ◽

Encapsulation Efficiency ◽

Tween 80 ◽

Span 80 ◽

Coa Reductase

Simvastatin is a cholesterol-lowering agent that inhibits the microsomal activity of 3-hydroxy-3-methylglutaril-CoA-reductase (HMG-CoA reductase), enzyme that contributes in biosynthesis cholesterol. Simvastatin has short half-life elimination about 2 hours and low solubility, this condition makes its bioavailability to be quite small. Simvastatin has adverse effect such as myopathy and rhabdomyolysis because of higher dose consumption of simvastatin. Controlled drug delivery system is needed to reduce the adverse effect. One of method that is used in drug delivery system is encapsulation using biodegradable polymer such as poly(L-lactic acid) and poly(ɛ-caprolactone). PLLA and PCL was blended with fix composition PLLA : PCL 60 : 40 (%w/w) by solvent evaporation technique using Tween 80 and Span 80 as emulsifier. Based on the optimization, the best encapsulation efficiency microcapsules were obtained at concentration of Tween 80 0.025% (v/v), Span 80 1% (v/v) with stirring speed at 900 rpm for 1 hour. The encapsulation efficiency was 83.67%. The best microcapsules were dissolved in dissolution media to get drug release profile. The percentage of drug release at pH 1.2 was 0.86% for 3 hours and in the phosphate buffer solution pH 7.4 for 12.22% for 52 hours.

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Pengembangan Dan Optimasi Formula Self Mikroemulsi Drug Delivery System (SMEDDS) Kurkumin Untuk Meningkatkan Bioavaibilitas

Jurnal Farmasi Indonesia ◽

10.31001/jfi.v14i2.294 ◽

2017 ◽

Vol 14 (2) ◽

pp. 99-109

Author(s):

Ilham Kuncahyo ◽

Pudiastuti RSP

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Curcuma Longa ◽

Drug Loading ◽

Tween 80 ◽

Lattice Design ◽

Peg 400 ◽

Anti Hiv

Kurkumin terbukti memiliki aktivitas sebagai anti-tumor, anti-inflamasi, anti-virus, anti-oksidasi dan anti HIV. Penggunaan kurkumin dalam proses pengobatan jangka panjang memberikan toksisitas yang rendah sehingga secara klinis akan sangat menguntungkan untuk dikembangkan. Kandungan aktif kurkumin yang berasal dari ekstrak tanaman curcuma longa ini mempunyai bioavaiblitas yang sangat rendah. Hal ini berkaitan karena kelarutan kurkumin yang jelek dalam air (11 ng/ml, pH 5,0) sehingga sedikit diserap di saluran pencernaan. Permasalahan ini dapat diatasi dengan membuat sediaan kurkumin dalam bentuk Self Mikroemulsi Drug Delivery System (SMEDDS) Penelitian awal dilakukan skrining terhadap kelarutan kurkumin dengan pembawa berbagai jenis minyak, surfaktan dan kosurfaktan. Hasil skrining dilanjutkan dengan pemilihan formula optimum SMEDDS kurkumin dengan menggunakan metode Simpelx Lattice Design (SLD). Tiga variabel akan memberikan 14 formula SMEDDS kurkumin yang masing-masing formula dilakukan pengujian terhadap karakteristiknya sebagai titik kritis meliputi : % transmitan, waktu emulsifikasi dan drug loading. Hasil masing-masing pengujian dianalisis datanya dengan Design Exspert versi 7 dan dilanjutnya validasi formula optimum dengan uji T dengan taraf kepercayaan 95%. Hasil penelitian menunjukkan bahwa skrining awal terhadap kurkumin didapatkan kelarutan yang terbesar pada jenis minyak zaitun, surfaktan Tween 80 dan kosurfaktan PEG 400. Ketiga jenis bahan ini dilakukan optimasi dengan SLD memberikan formula optimum komposisi SMEDDS kurkumin dengan komposisi 0,026 minyak zaitun ; 0,0913 Tween 80 dan 0,061 PEG 400.

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PENGEMBANGAN NANOPARTIKEL EKSTRAK DAUN KERSEN(Muntingia calabura.L) DENGAN TEKNIK SELF NANO EMULSIFYING DRUG DELIVERY SYSTEM (SNEDDS) UNTUK APLIKASI ANTIBAKTERI

Pharmaqueous : Jurnal Ilmiah Kefarmasian ◽

10.36760/jp.v1i2.91 ◽

2020 ◽

Vol 1 (2) ◽

pp. 27-34

Author(s):

Septiana Indratmoko ◽

Asep Nurrahman ◽

Axl Aprizal Herawan

Keyword(s):

Drug Delivery ◽

Staphylococcus Aureus ◽

Drug Delivery System ◽

Delivery System ◽

Drug Loading ◽

Tween 80 ◽

Peg 400

Kandungan flavonoid dan tanin pada daun kersen dapat menghambat pertumbuhan bakteri Staphylococcus aureus. Penelitian ini bertujuan untuk mengetahui pengaruh formulasi nanoemulsi daun kersen (Mutingia calabura.L) terhadap karakteristik nanoemulsi menggunakan teknik Self Nano Emulsifying Drug Delivery System (SNEDDS) dan pengaruhnya sebagai antibakteri Staphylococcus aureus. Ekstrak etanol daun kersen diformulasi dengan surfaktan, kosurfaktan dan minyak terpilih. Kemudian nanoemulsi ekstrak daun kersen diuji ukuran partikel, potensial zeta, drug loading dan stabilitas nanoemulsi. Nanoemulsi ekstrak etanol daun kersen dapat dihasilkan dengan formula Tween 80, PEG 400 dan VCO perbandingan 6:1:1. Ukuran partikel nanoemulsi 12,4 nm, potensial zeta 30,8 mV, drug loading yaitu 125 mg/ml dan stabil. Nanoemulsi ekstrak daun kersen dapat memberikan aktivitas antibakteri lebih baik daripada ekstrak daun kersen.

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