Use of Simplex Lattice Design in Development of Oral Self-Nanoemulsifying Drug Delivery System Containing Rosuvastatin Calcium

Oza, Nishant; Sagar, Swati; Khodakiya, Akruti

doi:10.22159/ijap.2020v12i3.34358

Cited by 6 publications

(11 citation statements)

References 13 publications

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“…A pseudo ternary phase diagram was created to identify efficient self-emulsification regions. In vitro diffusion studies revealed that the release of calcium rosuvastatin from SNEDDS was faster [28].…”

Section: Verification Of Optimal Snedds Formula Combination Of Mfgmentioning

confidence: 99%

Design and Characterization of Nanospray With Self-Nanoemulsifying Drug Delivery System Using Sinergistic Combination of Melastoma Malabathricum L. Fraction and Gentamicin

2021

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Objective: This study aimed to design a formula using Design-Expert software to obtain optimal Self-Nanoemulsifying Drug Delivery System (SNEDDS) formulas and to analyze nanospray characteristics of optimal SNEDDS. Methods: The study began with preparing ethanol extract from Melastoma malabathricum. The extract was then fractionated using ethyl acetate. The formulation design stage began with a solubility test of Melastoma malabathricum fraction and gentamicin (MFG) in various surfactants, co-surfactants and oils. Furthermore, the 14 formula of SNEDDS with various compositions of the selected surfactants, co-surfactants and oils were formulated and evaluated with pH response and emulsification time. Analysis was carried out using Design-Expert software with the simplex lattice design method in order to obtain the optimal formula profile. The pH, emulsification time, particle size, and zeta potential of the nanospray from SNEDDS optimal formulas were physically characterized. Stability of SNEDDS and the nanospray was then tested with freeze-thaw cycling and in vitro diffusion studies with Franz diffusion. Results: Based on the study, the ratios of optimal formula SNEDDS composition of Tween 80, propylene glycol, and soybean oil were 2.69: 2.64: 1.67 parts. Nanospray with SNEDDS technology had characteristics of pH 5.61±0.16, emulsification time 7.68±0.18, particle size 270.7 nm, and zeta potential-37.20 mV, and it was stable. Conclusion: Nanospray can be formulated from optimal SNEDDS using Design-Expert software. Nanospray with SNEDDS technology has physical characteristics and is stable. In vitro diffusion studies revealed that the release of Melastoma malabathricum from nanospray was faster than that without preparation.

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Section: Verification Of Optimal Snedds Formula Combination Of Mfgmentioning

confidence: 99%

Design and Characterization of Nanospray With Self-Nanoemulsifying Drug Delivery System Using Sinergistic Combination of Melastoma Malabathricum L. Fraction and Gentamicin

2021

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“…Beberapa fase minyak yang digunakan dalam formulasi SNEDDS meliputi capryol PGMC, minyak biji jintan hitam, asam oleat, minyak kelapa/VCO, capryol-90, olive oil, capryol-90, peceol, kombinasi peceol dan etiloleat, capmul MCM dan cremophor EL. [5][6][7][8][9][10][11]14,22,23 Suatu Surfaktan dapat menghasilkan nanoemulsi tipe minyak dalam air apabila memiliki HLB>10. 24 Surfaktan yang terlokalisasi pada droplet emulsi dapat menurunkan energi bebas antar muka dan menghasilkan barier terhadap koalesensi sehingga terjadi dispersi spontan secara termodinamika.…”

Section: Sneddsunclassified

“…25 kombinasi tween 20:labrasol (1:1), cremophor EL, cremophor 40, tween 20, labrasol, cremophor EL 300 dan acrysol K 140. [5][6][7][8][9][10][11]14 Ko-surfaktan berfungsi untuk meningkatkan fluiditas antar muka dengan cara penetrasi ke dalam film surfaktan. 13 Pemilihan fase minyak pada SNEDDS didasarkan pada kelarutan maksimal zat aktif dalam fase minyak, sedangkan pemilihan surfaktan dan ko-surfaktan berdasarkan pada kelarutan maksimum obat dalam surfaktan dan kosurfaktan serta efisiensi emulsifikasi terhadap fase minyak.…”

Section: Sneddsunclassified

“…Optimasi formulasi SNEDDS dapat menggunakan metode simplex lattice design dan box behnken design. [5][6][7][8][9][10][11][12][13][14] Pengembangan formulasi SNEDDS dapat meningkatkan bioavailabilitas oral, kelarutan dan permeabilitas intestinal. 15 Simplex lattice design (SLD) merupakan desain campuran dalam optimasi formulasi dengan syarat jumlah total bahan-bahan yang digunakan dalam formulasi selalu konstan.…”

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“…8,16 Metode SLD memungkinkan jumlah eksperimen optimasi formulasi yang sedikit. [8][9][10][11] Desain eksperimen lain yang dapat digunakan untuk optimasi formulasi SNEDDS adalah box behnken design (BBD) yang memiliki keunggulan dibandingkan desain penuh tiga level faktorial dan composite central design (CCD) karena lebih efisien dengan jumlah variabel yang sama namun jumlah percobaan yang dilakukan lebih sedikit sehingga dapat mereduksi biaya uji. 17 Pemanfaatan SLD dan BBD dalam optimasi formulasi meminimalkan jumlah percobaan dalam memperoleh formulasi SNEDDS yang optimal sehingga dapat menghemat biaya.…”

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Artikel Review: Optimasi Formulasi Snedds Dengan Simplex Lattice Design Dan Box Behnken Design

Akbar¹,

Nugroho²,

Martono³

2022

JFB

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SNEDDS merupakan campuran isotropik yang terdiri dari obat, surfaktan, ko-surfaktan dan minyak. Pengembangan dan optimasi formulasi yang tepat diperlukan untuk meminimalisir waktu, biaya, serta menjamin formulasi yang optimal. Tujuan dari penulisan artikel ini adalah untuk menjelaskan SNEDDS serta aplikasi simplex lattice design (SLD) dan box behnken design (BBD) dalam optimasi formulasi SNEDDS. Metode yang digunakan dalam menyusun review ini yaitu teknik studi pustaka dengan mencari literatur dalam bentuk data primer berupa jurnal nasional maupun jurnal internasional bahasa Inggris dalam 10 tahun terakhir (2011-2020). Optimasi formulasi SNEDDS dengan SLD dan BBD dilakukan dengan memilih formulasi yang memiliki nilai desirability lebih tinggi. Apabila respon terprediksi dan terukur pada formulasi SNEDDS optimal hasil prediksi SLD menunjukkan nilai p>0,05 pada one sample t-test, maka formulasi SNEDDS optimal dianggap valid. Kedekatan respon terukur dan terprediksi pada metode BBD dilakukan dengan menghitung nilai % bias. Beberapa penelitian menggunakan nilai persen bias (%) untuk mengukur kedekatan antara respon terprediksi dengan respon terukur dengan nilai persen (%) bias berkisar antara -6,04% - 7,3%. Nilai persen (%) bias yang semakin besar menunjukkan semakin besar penyimpangan antara respon terprediksi dengan respon terukur.

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Improved oral bioavailability of poorly water-soluble vorinostat by self-microemulsifying drug delivery system

Janakiraman

Islam

Liew

et al. 2022

Beni-Suef Univ J Basic Appl Sci

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Background Vorinostat is a histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA) with anticancer properties. However, it is plagued by low water solubility, low permeability (BCS class IV drug), and suboptimal pharmacokinetics. The purpose of the present study was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of vorinostat. Capryol 90, labrasol, and polyethylene glycol (PEG 400) were selected as oil phase, surfactant, and co-surfactant, respectively. The vorinostat self-microemulsifying drug delivery systems were tested for self-microemulsifying time, phase separation, effect of pH, droplet size, zeta potential, dilution study, Fourier-transform infrared (FT-IR) spectroscopy analysis, and field emission scanning electron microscopy (FESEM). A rat model in vivo pharmacokinetic study was conducted for the optimized formulation against vorinostat pure drug powder. Results The results from the characterization studies showed that the optimized formulation (F7) self-microemulsification time was 1.4 ± 0.05 min and no precipitation or phase separation was observed. The mean droplet size, polydispersity index (PDI), and zeta potential of the optimized formulation (F7) were found to be 272.9 ± 82.7 nm, 0.415, and − 57.2 mV, respectively. The pharmacokinetic parameters of the optimized formulation (F7) showed a 1.6-fold increase in maximum concentration (Cmax) and a 3.6-fold increase in area under the curve (AUC(0−∞)), in comparison with pure drug in suspension. Conclusions The findings suggest that SMEDDS formulation could be an effective method for increasing the oral bioavailability of vorinostat, which is poorly water soluble.

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Use of Simplex Lattice Design in Development of Oral Self-Nanoemulsifying Drug Delivery System Containing Rosuvastatin Calcium

Cited by 6 publications

References 13 publications

Design and Characterization of Nanospray With Self-Nanoemulsifying Drug Delivery System Using Sinergistic Combination of Melastoma Malabathricum L. Fraction and Gentamicin

Design and Characterization of Nanospray With Self-Nanoemulsifying Drug Delivery System Using Sinergistic Combination of Melastoma Malabathricum L. Fraction and Gentamicin

Artikel Review: Optimasi Formulasi Snedds Dengan Simplex Lattice Design Dan Box Behnken Design

Improved oral bioavailability of poorly water-soluble vorinostat by self-microemulsifying drug delivery system

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