scholarly journals Formulation and Optimization of Furosemide Snedds With Variation Concentration of Tween 80 and PEG 400

2021 ◽  
Vol 2 (1) ◽  
pp. 34-42
Author(s):  
Sesilia Putri Nandita ◽  
Ilham Kuncahyo ◽  
Reslely Harjanti
Keyword(s):  
Particle Size ◽  
Drug Loading ◽  
Tween 80 ◽  
In Vitro Dissolution ◽  
Lattice Design ◽  
Peg 400 ◽  
Simplex Lattice Design ◽  
Simplex Lattice ◽  
Optimum Formula

Furosemide is a potent diuretic drug that has low bioavailability. Furosemide can be formulated into nanoemulsion preparations using the SNEDDS method to increase its bioavailability as SNEDDS can form stable nanoemulsions with droplet sizes 200 nm. This study aims to identify the optimum formula for variations in the concentration of surfactant Tween 80 and cosurfactant PEG 400 based on the characterization tests of emulsification time, percent transmittance, and drug loading. The independent variables used in this study were Tween 80 and PEG 400. Seven furosemide SNEDDS formulas from the Simplex Lattice Design (SLD) method were tested for characterization in the form of emulsification time, percent transmittance, and drug loading. The characterization results were optimized using Simplex Lattice Design. The optimum formula was re-characterized, including emulsification time, percent transmittance, drug loading, particle size, zeta potential, and in vitro dissolution. The results were then compared with theoretical values and analyzed using the One-Sample T-test method. Optimization results showed Tween of 61.4922% and PEG 400 of 18.5078% with the characterization of emulsification time 15.25 seconds, percentage transmittance 94.20%, drug loading 50 100.2 ppm, particle size 12.18 nm. Furthermore, the zeta potential was -17.6 mV, and the in vitro dissolution rate reached 106.71% within 15 minutes.

scholarly journals OPTIMASI FORMULA SELF NANO EMULSIFYING DRUG DELIVERY SYSTEM (SNEDDS) EKSTRAK ETANOL DAUN SIRSAK (Annona muricata) SEBAGAI ANTIBAKTERI (Stapylococcus aureus) DENGAN METODE SIMPLEX LATTICE DESIGN

2021 ◽  
Vol 2 (1) ◽  
pp. 125-134
Author(s):  
Septiana Indratmoko Indratmoko
Keyword(s):  
Drug Delivery ◽  
Staphylococcus Aureus ◽  
Drug Loading ◽  
Tween 80 ◽  
Annona Muricata ◽  
Paired Sample ◽  
Lattice Design ◽  
Peg 400 ◽  
Simplex Lattice Design ◽  
Simplex Lattice

Ekstrak daun sirsak (Annona Muricata) memilki kandungan senyawa metabolit sekunder yang bersifat sebagai antibakteri diantaranya yaitu flavonoid, alkaloid, tanin dan saponin. Pemanfaatan ekstrak daun sirsak diformulasikan dalam sediaan SNEDDS untuk meningkatkan kelarutan sehingga tercapai efek terapi yang maksimal. Tujuan penelitian ini adalah untuk mengetahui formula optimum SNEDDS ekstrak daun sirsak berserta uji sifat fisik dan efektivitasnya terhadap bakteri Staphylococcus aureus. Penggunaan nanoemulsi dioptimalkan dengan menggunakan Simplex Lattice Design sehingga didapatkan perbandingan formulasi terbaik (tween 80) 6 : (PEG 400) 1 : (Minyak terpilih) 1 dengan nilai desirability 0,987 dengan drug loading ekstrak sebesar 25 mg/mL. Parameter uji sifat fisik SNEDDS diperoleh pengamatan stabilitas sediaan stabil, nilai transmitan 97,7%, emulsification time 3 menit dan pH sebesar 6. Uji aktivitas antibakteri sediaan SNEDDS ekstrak daun sirsak memiliki daya hambat lebih besar daripada ekstrak daun sirsak murni. Hasi uji efektivitas antibakteri dianalisis dengan paired sample t-test memiliki signifikasi < 0,05 sehingga ada perbedaan antar kelompok.

scholarly journals Formulation and evaluation of self nano-emulsifying drug delivery system of ezetimibe for dissolution rate enhancement

2020 ◽  
Vol 11 (2) ◽  
pp. 1294-1301
Author(s):  
Geethanjali K ◽  
Vaiyana Rajesh C
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Dissolution Rate ◽  
Delivery System ◽  
Tween 80 ◽  
In Vitro Dissolution ◽  
Cinnamon Oil ◽  
Peg 400 ◽  
Solid Form

The present study was aimed to develop a Self Nano Emulsifying Delivery System of Ezetimibe (EZM) for enhancing its dissolution rate. Ezetimibe is a cholesterol absorption inhibitor, being a lipophilic drug due to its low solubility EZM shows a low dissolution profile. The SNEDDS formulation consisted of excipients Cinnamon oil, Tween 80, PEG 400 as the Oil, Surfactant and Co-surfactant. Twelve formulations with different ratios of Oil, Surfactant and Co-surfactant were prepared. The liquid SNEDDS were then converted into Solid form by adsorption technique using Avicel PH 101 and Aerosil 200 as adsorbents. The liquid SNEDDS was characterised for Particle size, Emulsification time, Dispersibility, percentage transmittance, PCM, Centrifugation, Cloud Point and Freeze thaw cycle. The solid form was characterized for the flow property, SEM, Drug content and in-vitro dissolution. Among the twelve formulations F6 formulation was found to have a particle size of 196 nm and PDI of 0.123. F6 formulation was selected as the best and it was made into solid by adsorption onto solid carriers. The F6 formulation consisted of the 25% Cinnamon oil, 50% tween 80 and 25% PEG 400. The in-vitro dissolution rate of the prepared formulation was compared with the marketed formulation. The in-vitro dissolution data showed that the drug release at the end of 60 mins from marketed formulation was 63.75 % and from SNEDDS formulation was         90.62 %. The dissolution rate of the prepared SNEDDS was increased by 1.42 times than the marketed formulation. The increase in the dissolution rate shows that SNEDDS is a suitable drug delivery system to enhance the rate of dissolution of Ezetimibe.

Self-Nanoemulsifying Drug Delivery System (SNEDDS) with Enhanched Solubilization of Ethanol Extract from Mangosteen Peels (Garcinia Mangostana, L.) for Treatment of Topical Gangrene Foot: Design and Optimization

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
Pratiwi L. ◽  
Sari R. ◽  
Apridamayanti P.
Keyword(s):  
Drug Delivery ◽  
Ph Value ◽  
Drug Loading ◽  
Coconut Oil ◽  
Ethanol Extract ◽  
Garcinia Mangostana ◽  
Lattice Design ◽  
Peg 400 ◽  
Simplex Lattice Design ◽  
Simplex Lattice

The aim of the present study is to develop and optimize self-nanoemulsifying drug delivery systems (SNEDDS) to improve the topical bioavailability of poorly soluble ethanol extract of mangosteen peels and to get optimum method of SNEDDS by simplex lattice design, using Design Expert software ®version 7. Solubility of ethanol extract of the mangosteen peels was estimated in various compositions to select proper components combinations. Virgin coconut oil/ VCO (oil), Tween® 80 (surfactants) as well as polietilenglikol 400 (PEG 400) (co-surfactants) were employed to construct pseudo-ternary phase diagrams. Transmittance and pH, droplet size, zeta potential, and thermodynamic stability were performed to optimize formulations from phase diagram. Fourteen formulations composed of VCO, Tween 80 and PEG 400 at simplex lattice design ratios were selected. The results showed that the ethanol extract of the mangosteen peels SNEDDS optimum consisting of Cremophor EL as the surfactant, PEG 400 as the co-surfactant, and VCO as the oil phase with a ratio of 5.27: 1: 1.72. Evaluation of SNEDDS with an optimum formulation with drug loading value of 125 mg/5 mL, emulsification time of 5,2 seconds, transmittance value of 74,6552 %, pH value 5,85 and has a particle size of 18,9 nm. Ethanol extract of the mangosteen peels loaded SNEDDS, with enhanced solubilization and nanosizing, and has potential to improve the absorption of drug and increase its topical antimicrobial activity against Staphylococcus aureus.

scholarly journals Optimasi Formulasi Esens Sheet Mask Kombinasi Ekstrak Spirulina platensis dan Nanopartikel Bentonit dengan Metode Simplex Lattice Design

2019 ◽  
Vol 16 (1) ◽  
pp. 18-27
Author(s):  
Erindyah Retno Wikantyasning ◽  
Ulil Fikri Nurhakimah ◽  
Ramadhani Dwi Sula ◽  
Kartika Fidi Astuti
Keyword(s):  
Antioxidant Activity ◽  
Particle Size ◽  
Spirulina Platensis ◽  
Physical Stability ◽  
Tween 80 ◽  
High Energy ◽  
Lattice Design ◽  
Nanoparticles Characterization ◽  
Simplex Lattice ◽  
Optimum Formula

Spirulina platensis contained phycocyanin that has the potential for antioxidant activity. Bentonite contains various minerals that can absorb water and was known having ability for scavenging of free radicals. The purpose of this study was to obtain the optimum formulae of sheet mask essence, containing combination of Spirulina platensis extract and bentonite nanoparticles and evaluated the antioxidant activity using DPPH (2,2-diphenyl-1-pikrihidrazil) assay. Bentonite nanoparticles was prepared by High Energy Milling (HEM) method and characterized using Particle Size Analyzer (PSA). The results of the nanoparticles characterization was 152,8±0,69 nm for the particle size and 0.106±0.03 for PI value. Physical stability tests showed that the formula was homogenous, viscosity between 0.7-1.1 dPas, and pH between 5-6.5. The IC50 value of Spirulina platensis extract was 256.46 ppm with AAI category was medium. The antioxidant test of this fomula that contain Spirulina platensis extract and bentonite nanoparticles did not show any potential antioxidant activity. The concentrations of PEG 400 and Tween 80 were used to formulate the optimum formula were 4.29% w/w and 6.71% w/w.

scholarly journals Formulasi dan Karakterisasi SNEDDS Ekstrak Jinten Hitam (Nigella Sativa) dengan Fase Minyak Ikan Hiu Cucut Botol (Centrophorus Sp) serta Uji Aktivitas Imunostimulan

2018 ◽  
Vol 3 (1) ◽  
pp. 50 ◽  
Author(s):  
Maya Uzia Beandrade
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Nigella Sativa ◽  
Tween 80 ◽  
Sprague Dawley ◽  
Design Expert ◽  
Lattice Design ◽  
Peg 400 ◽  
Simplex Lattice Design ◽  
Simplex Lattice

<p>Jinten hitam (<em>Nigella sativa</em>) mengandung senyawa timokuinon yang berefek sebagai imunostimulan. Ekstrak jinten hitam dikembangkan menjadi SNEDDS (<em>Self-nanoemulsifying Drug Delivery System</em>) karena masalah kelarutan. Penelitian dilakukan untuk mengetahui karakteristik SNEDDS ekstrak jinten hitam yang meliputi viskositas, ukuran tetesan nanoemulsi, <em>extract loading</em>, dan stabilitas. Pengujian aktivitas imunostimulan SNEDDS meliputi rasio sel makrofag dan indeks fagositosis.</p><p>SNEDDS ekstrak jinten hitam dioptimasi dengan metode <em>Simplex Lattice Design</em> menggunakan <em>Design Expert 7.1.5., </em>selanjutnya SNEDDS optimal diuji ukuran tetesan nanoemulsi dan zeta potensial, viskositas, serta uji stabilitas. Uji aktivitas imunostimulan dilakukan dengan metode <em>biolatex assay</em> terhadap tikus <em>Sprague Dawley</em> sebanyak 5 tikus/kelompok selama 15 hari dengan pemberian satu kali sehari yaitu kontrol positif (ekstrak meniran 7,2 mg/tikus), kelompok perlakuan yaitu ekstrak jinten hitam dengan dosis 200 mg/kgBB serta SNEDDS ekstrak jinten hitam (200 mg/kgBB), kelompok plasebo berupa formula SNEDDS tanpa ekstrak jinten hitam, dan kontrol normal, selanjutnya dihitung rasio dan indeks fagositosis makrofag.</p>SNEDDS ekstrak jinten hitam optimal mengandung 15% minyak ikan hiu cucut botol, 67,344% surfaktan (10,102% croduret 50 ss dan 57,242% tween 80), 17,656% PEG 400 sebagai ko-surfaktan dengan hasil ukuran tetesan nanoemulsi 16,3 nm, PI sebesar 0,202, zeta potensial -43,5 mV, dan viskositas antara 234,69 – 255,71 cP. Hasil <em>extract loading</em> sistem SNEDDS mencapai 600 mg ekstrak/g sistem. SNEDDS stabil setelah penyimpanan selama 90 hari pada suhu kamar dan uji <em>freeze-thawing</em>. SNEDDS ekstrak jinten hitam dengan dosis 200 mg/kgBB dapat meningkatkan rasio sel makrofag dan indeks fagositosis dibandingkan dengan ekstrak jinten tanpa formulasi (P&lt;0,05).

scholarly journals In vitro and in vivo Evaluation of Ibuprofen Nanosuspensions for Enhanced Oral Bioavailability

2021 ◽  
Author(s):  
Mohsen Hedaya ◽  
Farzana Bandarkar ◽  
Aly Nada
Keyword(s):  
Particle Size ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
In Vivo Evaluation ◽  
Poorly Soluble ◽  
Extent Of Absorption ◽  
Better Than

Introduction: The objectives were to prepare, characterize and in vivo evaluate different ibuprofen (IBU) nanosuspensions prepared by ultra-homogenization, after oral administration to rabbits. Methods: The nanosuspensions produced by ultra-homogenization were tested and compared with a marketed IBU suspension for particle size, in vitro dissolution and in vivo absorption. Five groups of rabbits received orally 25 mg/kg of IBU nanosuspension, nanoparticles, unhomogenized suspension, marketed product and untreated suspension. A sixth group received 5 mg/kg IBU intravenously. Serial blood samples were obtained after IBU administration. Results: The formulated nanosuspensions showed significant decrease in particle size. Polyvinyl Pyrrolidone K30 (PP) was found to improve IBU aqueous solubility much better than the other tested polymers. Addition of Tween 80 (TW), in equal amount as PP (IBU: PP:TW, 1:2:2 w/w) resulted in much smaller particle size and better dissolution rate. The Cmax achieved were 14.8±1.64, 11.1±1.37, 9.01±0.761, 7.03±1.38 and 3.23±1.03 μg/ml and the tmax were 36±8.2, 39±8.2, 100±17.3, 112±15 and 105±17 min for the nanosuspension, nanoparticle, unhomogenized suspension, marketed IBU suspension and untreated IBU suspension in water, respectively. Bioavailability of the different formulations relative to the marketed suspension were the highest for nanosuspension> unhomogenized suspension> nanoparticles> untreated IBU suspension. Conclusion: IBU/PP/TW nanosuspensions showed enhanced in vitro dissolution as well as faster rate and higher extent of absorption as indicated from the higher Cmax, shorter tmax and larger AUC. The in vivo data supported the in vitro results. Nanosuspensions prepared by ultra-high-pressure-homogenization technique can be used as a good formulation strategy to enhance the rate and extent of absorption of poorly soluble drugs.

scholarly journals Preparation and evaluation of an ispaghula based directly compressible matrixing agent for controlled release

2008 ◽  
Vol 58 (3) ◽  
pp. 309-316 ◽  
Author(s):  
Anita Lalwani ◽  
Jolly Parikh
Keyword(s):  
Controlled Release ◽  
Hydroxypropyl Methylcellulose ◽  
Hydrogen Phosphate ◽  
Lattice Design ◽  
Phosphate Dihydrate ◽  
Simplex Lattice Design ◽  
Dependent Variables ◽  
Simplex Lattice ◽  
Preparation And Evaluation

Preparation and evaluation of an ispaghula based directly compressible matrixing agent for controlled releaseThe objective of the present investigation was to prepare and evaluate an ispaghula husk based directly compressible (DC) adjuvant that can be used as matrixing agent using an agglomeration technique. Addition of hydroxypropyl methylcellulose was found necessary to improve cohesion. Lactose (X1), calcium hydrogen phosphate dihydrate (X2) and Avicel PH101 (X3), used along with ispaghula in preparation of agglomerates, were selected as three independent variables in a simplex lattice design affecting compressional and dissolution characteristics of the drug from the DC adjuvant. The agglomerates were evaluated for their flow properties. Tablets were prepared using 70% agglomerates and 30% acetaminophen, a poorly compressible drug, and were subjected toin vitrodrug release study. Amounts of the drug released at the end of 60 min (Y60), 300 min (Y300) and 480 min (Y480) were selected as dependent variables in a simplex lattice design. Batch IH05 that contained lactose and calcium hydrogen phosphate dihydrate in a 1:2 ratio could control the release for 12 hours and thus form the basis for twice a-day-dosing.

scholarly journals Optimasi Formula dan Uji Aktivitas Secara In Vitro Lotion O/W Ekstrak Etanolik Rimpang Temu Mangga (Curcuma Mangga Val. dan van Zijp) sebagai Tabir Surya

2018 ◽  
Vol 14 (1) ◽  
pp. 29 ◽  
Author(s):  
Mercy Arizona ◽  
A. Karim Zulkarnain
Keyword(s):  
Freeze Thaw ◽  
Lattice Design ◽  
Simplex Lattice Design ◽  
Simplex Lattice ◽  
One Way Anova

Ekstrak temu mangga (Curcuma mangga Val.) memiliki aktivitas sebagai tabir surya secara spektrofotometri. Penelitian ini bertujuan untuk mengetahui formula optimum lotion o/w, sifat dan stabilitas fisik formula optimum lotion o/w, serta aktivitas tabir surya formula optimum lotion o/w ekstrak temu mangga  (Curcuma mangga Val.) secara spektrofotometri. Formula optimum diperoleh dengan metode Simplex Lattice Design (SLD). Respon yang digunakan untuk menentukan formula optimum adalah daya lekat dan viskositas. Stabilitas fisik lotion o/w pada suhu ruang meliputi uji daya sebar, daya lekat, dan viskositas, serta uji freeze thaw cycling. Aktivitas tabir surya lotion o/w ditentukan secara spektrofotometri untuk menentukan Sun Protecting Factor (SPF), % transmisi eritema, dan % transmisi pigmentasi. Data dianalisis dengan One Way ANOVA dan uji t. Hasil penelitian menunjukkan bahwa formula optimum lotion o/w pada kombinasi 5% trietanolamin (TEA)-stearat dan 5% setil alkohol. Lotion o/w ekstrak temu mangga memiliki memiliki daya sebar 63,21±2,69 cm2, daya lekat 2,32±0,15 detik, dan viskositas sebesar 133,5±8,05 dPas. Hasil analisis statistika menunjukkan bahwa lotion o/w smemiliki stabilitas yang baik. Lotion o/w mempunyai aktivitas sebagai tabir surya pada konsentrasi lotion o/w 12,5% yang ditunjukkan dengan nilai SPF sebesar 12,82±0,16 dan tidak efektif dalam perlindungan terhadap eritema dan pigmentasi.

scholarly journals Optimasi Formula Tablet Piroksikam Menggunakan Eksipien Laktosa, Avicel pH-101, dan Amprotab dengan Metode Simplex Lattice Design

2020 ◽  
Vol 17 (1) ◽  
pp. 31-44
Author(s):  
Ikhwan Yuda Kusuma ◽  
Rani Prabandari
Keyword(s):  
Physical Properties ◽  
Design Method ◽  
Dominant Factor ◽  
Content Uniformity ◽  
Compression Tests ◽  
Lattice Design ◽  
Simplex Lattice Design ◽  
Contour Plots ◽  
Simplex Lattice ◽  
Optimum Formula

Piroxicam solubility in water is very small this cause problem in the process of absorption so that it’s required an optimal formula to establish the physical properties of tablet quality for piroxicam tablets. The purpose of this research was creating formulas with the optimal combination of excipients lactose, Avicel pH 101, and piroxicam amprotab to obtain tablets with good physical properties and disolution. Seven piroxicam tablet formulas were made with a combination of lactose, avicel PH-101, and Amprotab on 2 batches. Method for making tablets piroxicam was established by direct compression. Tests included were the physical properties of piroxicam tablets tablets weight uniformity, uniformity of size, hardness, brittleness, disintegration test, as well as dissolution test, and content uniformity. Based on the simplex lattice design method, lactose is a dominant factor to improved the uniformity of tablet’s concentartions. Interaction of two components avicel PH-101 and amprotab is a dominant factor to reduced vulnerability. Interaction of three components lactose, avicel PH-101 and amprotab is a dominant factor to lowered the value coefisien variation of weight uniformity, increased hardness, decreased the disintegration, and improved dissolution of tablets. Selection of the optimum formula was determined by the method of simplex lattice design through diagrams superimposed contour plots and contour plots for obtaining the optimal proportions of each ingredient as follows: lactose (85,154–100%), avicel PH-101 (0–12,437%), and amprotab (0–5,425%).

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