scholarly journals FORMULATION AND EVALUATION OF ATORVASTATIN CALCIUM NANOCRYSTALS CONTAINING P-GLYCOPROTEIN INHIBITORS FOR ENHANCING ORAL DELIVERY

2021 ◽  
pp. 19-23
Author(s):  
SARAH LABIB ◽  
MOHAMED NASR ◽  
MOHAMED NASR
Keyword(s):  
Polyethylene Glycol ◽  
Oral Drug Delivery ◽  
Tween 80 ◽  
Degree Of Crystallinity ◽  
Oral Drug ◽  
Tween 20 ◽  
Atorvastatin Calcium ◽  
Peg 400 ◽  
P Glycoprotein ◽  
Saturated Solubility

Objective: The main objective of this study was to develop atorvastatin calcium (ATR) as an oral drug delivery system for a P-glycoprotein (P-gp) substrate drug using different pharmaceutical excipients that inhibit P-glycoprotein and evaluate the influence of nanocrystals on the dissolution characteristics and bioavailability compared to the plain drug. Methods: A nanosuspension was prepared by Solvent-antisolvent precipitation method using a solvent containing stabilizer that act as a p-gp inhibitor dissolved in distilled water as polyethylene glycol 300, polyethylene glycol 400 (PEG 300, PEG 400), tween 20 and tween 80 while the solvent selected for atorvastatin calcium was methanol. The concentrations were as follows: PEG 300 and 400 = 0.25% w/v, tween 20 and 80 = 0.75% v/v. Nanocrystals were extracted from the suspension and characterized. Results: Particle size of the drug was 1307±127.79 nm while the formulas prepared ranged from 223±17.67 to 887±58.12 nm. Pure ATR had a saturated solubility of 0.059±0.005 mg/ml and the prepared nanocrystals ranged from 0.32±0.021 to 0.88±0.019 mg/ml. The Percentage of drug released of plain atorvastatin calcium reached 41.49% while the formula ranged from 44.32 to 61.5%. Both XRD and SEM discussed the degree of crystallinity as follows: F1<F2<F4<F3<ATR. Conclusion: 0.3% of PEG 300 and PEG 400 were not enough to formulate proper nanocrystals while 0.75% tween 20 and tween 80 achieved acceptable formulas. F4 which is prepared with tween 80 exhibited the highest enhancement in saturated solubility, dissolution rate and subsequently expected to have improved oral bioavailability.

scholarly journals FORMULATION AND CHARACTERIZATION OF LAFUTIDINE NANOSUSPENSION FOR ORAL DRUG DELIVERY SYSTEM

2018 ◽  
Vol 10 (2) ◽  
pp. 20 ◽  
Author(s):  
Noor Mohammed Dawood ◽  
Shaimaa Nazar Abdal-hammid ◽  
Ahmed Abbas Hussien
Keyword(s):  
Particle Size ◽  
Fourier Transforms ◽  
Oral Drug Delivery ◽  
In Vitro Release ◽  
Tween 80 ◽  
Precipitation Method ◽  
Oral Drug ◽  
Tween 20 ◽  
Dissolution Profile ◽  
Particle Size Reduction

Objective: The objective of this study was to prepare nanosuspension of a practical water insoluble antiulcer drug which is lafutidine to enhance the solubility, dissolution rate with studying the effect of different formulation variables to obtain the best formula with appropriate physical properties and higher dissolution rate.Methods: Nanosuspension of lafutidine was prepared using solvent anti-solvent precipitation method using Polyvinylpyrrolidone K-90(PVP K-90) as the stabilizer. Ten formulations were prepared to show the effect of different variables in which two formulations showed the effect of stabilizer type, three formulations showed the effect of stabilizer concentration, two formulations showed the effect of combination of polymer with surfactant such as tween 80, three formulations show the effect of stirring speed and three formulations prepare to show the effect of addition of co-surfactant such as tween 20. All these formulations are evaluated for their particle size and entrapment efficiency and in vitro release. The selected one was evaluated for zeta potential, scanning electron microscope, atomic force microscopy, Fourier transforms infrared spectroscopy, differential scanning calorimetry, saturation solubility and stability study.Results: The formulations (F3-F10) were in the nano size. The optimum concentration of the stabilizer was in the formulation when the drug: polymer: surfactant ratio 1:4:4 and the optimum stirring speed was 1500 rpm. Dramatic effect on the particle size reduction was found by the addition of co-surfactant (tween 20) in formulation F7 that has a particle size 15.89±1.8 nm. The selected formula F7 showed an enhanced dissolution profile (10 min) compared to the pure drug at all-time intervals.Conclusion: The results show that the formulation that contains drug: PVP-K90: tween 80: tween 20 in ratio 1:4:2:2 is the best one and can be utilized to formulate lafutidine nanosuspension. 

Solubility Studies and Validation of Lovastatin using High Performance Liquid Chromatography Method

2021 ◽  
pp. 6285-6288
Author(s):  
Nurhabibah Nurhabibah ◽  
A.K. Nugroho ◽  
Ronny Martien ◽  
Endang Lukitaningsih
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
Oleic Acid ◽  
High Performance ◽  
Tween 80 ◽  
Tween 20 ◽  
Chromatography Method ◽  
Peg 400 ◽  
Solubility Studies ◽  
Liquid Chromatography Method

This study aimed to determine the solubility of lovastatin (LV) in different oil, surfactant, and co-surfactant using the high-performance liquid chromatography method. LV was solubility studies in different vehicle. The different vehicle used almond oil, sunflower oil, oleic acid, olive oil, soybean oil, and corn oil, isoprophyl myristate, myoglyol, tween 80, tween 20, and cremophor R.H. 40, propylene glycol, and PEG 400. Each of them was added lovastatin until saturated. The mixtures were mixing, sonicating, putting in the water bath and standing for 24 hours, then centrifugated. Each of the aliquot 2 µL diluted with acetonitrile and determination of concentration lovastatin using HPLC, with detector ultraviolet at 237 nm. Before determinate LV validated, and curve calibration at range 2-16 µg/mL was made. This study using the HPLC method with detector UV 237 nm, Agilent C 18 (4.6 x 150 mm 5 µ) column, and acetonitrile: water (70:30 v/v) as mobile phase. Calibration curve of lovastatin at the range 2-16 µg/mL with linear regression 0.999. Accuracy and precision showed that. Lovastatin has high soluble in oleic acid, tween 80, and PEG 400.

Effect Of Surfactant Chain Length On Emulsification Dynamics Of Self Emulsifying Formulation Of Poorly Soluble Drug

2021 ◽  
Vol 18 ◽  
Author(s):  
Shailendra Chouhan ◽  
Lalit Singh Chauhan
Keyword(s):  
Chain Length ◽  
Tween 80 ◽  
Tween 20 ◽  
Almond Oil ◽  
Peg 400 ◽  
Globule Size ◽  
Poorly Soluble ◽  
Tween 40 ◽  
Poorly Soluble Drug ◽  
Tween 60

Aim: In this work the aim was to study the chain length of surfactant on the self emulsifying system of a poorly soluble drug, aceclofenac. The selection of almond oil as a lipid vehicle was done on basis of solubility and compatibility of the vehicle with the drug. Methods: The effect of varying chain length of different surfactants of Tween series namely Tween 20, Tween 40, Tween 60 and Tween 80 was evaluated on self emulsifying efficiency by constructing pseudoternary diagrams. PEG-400 was used as co-surfactant in a definite ratio with all the surfactants to minimize their concentration. The best self emulsifying ability was exhibited by Tween 80: PEG-400 combination followed by Tween 60: PEG-400, Tween 40: PEG-400, Tween 20: PEG-400. This observation indicates that as the chain length of Tweens increases their ability to form a good microemulsion increases if same co-surfactant is used. Results: However it has also been found that the presence of unsaturated bond in Tween 80 provides it an elasticity which supports good intermixing of oil and water and leading to formation of a fine microemulsion. Six different formulations were prepared using combination of almond oil, Tween 80, PEG-400 and the drug aceclofenac. Conclusion : The formulations were subjected to various evaluation parameters such as dispersibility, transmittance, pH, globule size, polydispersibility, zeta potential, viscosity, refractive index and in vitro dissolution. The best formulation was found to have globule size of less than 100 nm, zeta potential of -3.35 ± 0.60 mV which indicates formation of a microemulsion of aceclofenac with good stability.

scholarly journals Skrining Berbagai Jenis Surfaktan Dan Kosurfaktan Sebagai Dasar Pemilihan Formulasi Nanoemulsi

2021 ◽  
Vol 1 (3) ◽  
pp. 158-166
Author(s):  
Ni Luh Putu Karunia Vidya Nirmalayanti
Keyword(s):  
Phase Diagram ◽  
Propylene Glycol ◽  
Research Method ◽  
Tween 80 ◽  
Tween 20 ◽  
Peg 400 ◽  
Tween 60 ◽  
Main Components ◽  
Optimum Formula ◽  
Pseudoternary Phase Diagram

The main components for making nanoemulsions are oil, surfactants, and cosurfactants. Before formulating nanoemulsions, screening the surfactants and cosurfactants is necessary to produce an optimum formula. Thus, it carries out surfactants screening, namely (tween 20, tween 60, tween 80) and cosurfactants (propyleneglycol, PEG 400, glycerin). This study aimed to screen suitable selection and cosurfactants as the basis for making nanoemulsions. Then, the research method was carried out in two ways: surfactant screening and cosurfactant screening. The final results were analyzed using a pseudoternary phase diagram. The surfactant screening results were tween 20 (40mL), tween 60 (40mL), tween 80 (60mL); thereby, the best surfactant candidate was tween 80. The results of the surfactant screening on the pseudoternary phase diagram are the most optimal, namely tween 80 with propylene glycol because it has a large nanoemulsion formation area. The study proposed the ratio of oil: smix (tween 80 and propyleneglycol) (1:9) as the optimum formula used to make a nanoemulsion base.

scholarly journals Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19

2021 ◽  
Vol 23 (1) ◽  
Author(s):  
Dina B. Mahmoud ◽  
Mohamed Mofreh Bakr ◽  
Ahmed A. Al-karmalawy ◽  
Yassmin Moatasim ◽  
Ahmed El Taweel ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Mixed Micelles ◽  
Oral Drug Delivery ◽  
Ex Vivo ◽  
Tween 80 ◽  
Pluronic F127 ◽  
Oral Drug ◽  
Simple Method ◽  
Oral Drug Delivery System ◽  
Preclinical And Clinical Studies

AbstractInvestigating bicelles as an oral drug delivery system and exploiting their structural benefits can pave the way to formulate hydrophobic drugs and potentiate their activity. Herein, the ability of non-ionic surfactants (labrasol®, tween 80, cremophore EL and pluronic F127) to form curcumin loaded bicelles with phosphatidylcholine, utilizing a simple method, was investigated. Molecular docking was used to understand the mechanism of bicelles formation. The % transmittance and TEM exhibited bicelles formation with labrasol® and tween 80, while cremophor EL and pluronic F127 tended to form mixed micelles. The surfactant-based nanostructures significantly improved curcumin dissolution (99.2 ± 2.6% within 10 min in case of tween 80-based bicelles) compared to liposomes and curcumin suspension in non-sink conditions. The prepared formulations improved curcumin ex vivo permeation over liposomes and drug suspension. Further, the therapeutic antiviral activity of the formulated curcumin against SARS-CoV-2 was potentiated over drug suspension. Although both Labrasol® and tween 80 bicelles could form bicelles and enhance the oral delivery of curcumin when compared to liposomes and drug suspension, the mixed micelles formulations depicted superiority than bicelles formulations. Our findings provide promising formulations that can be utilized for further preclinical and clinical studies of curcumin as an antiviral therapy for COVID-19 patients.

scholarly journals Formulation and evaluation of atorvastatin calcium niosomes

2021 ◽  
Vol 2 (1) ◽  
pp. 116-126
Author(s):  
Neha Rani ◽  
Rupali Rana ◽  
Reena Thakur ◽  
Shivali Singla ◽  
Sachin Goyal
Keyword(s):  
Drug Delivery ◽  
Oral Bioavailability ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Drug Carriers ◽  
Tween 20 ◽  
Atorvastatin Calcium ◽  
Span 60

Atorvastatin calcium is a HMG-CoA reductase inhibitor used for the treatment of hyperlipidaemia. It has oral bioavailability of ≤12 %. It also undergoes high first pass metabolism. It is highly soluble in acidic pH and absorbed more in the upper part of the gastrointestinal tract. In order, to improve the absorption and its oral bioavailability, niosomes of Atorvastatin calcium have been formulated and evaluated on different parameters. Niosomes play an increasingly important role in drug delivery as they can reduce toxicity and 000000000modify pharmacokinetic and bio-availability. Niosomes formulations of Atorvastatin calcium were successfully developed by thin film hydration technique using nonionic surfactant i.e. Span 40, Span 60 Span 80, Tween 20, Tween 40, Tween 80 and cholesterol at different concentrations. The formulations were evaluated for size, shape, and entrapment efficiency. In-vitro release and stability studies also performed. Results indicated that Niosomes were prepared succesfully work as promising drug carriers and promising drug delivery module.

scholarly journals Effect of Polyethylene Glycol Content and Molar Mass on Injection Molding of Hydroxypropyl Methylcellulose Acetate Succinate-Based Gastroresistant Capsular Devices for Oral Drug Delivery

Polymers ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 517 ◽  
Author(s):  
Francesco Briatico-Vangosa ◽  
Alice Melocchi ◽  
Marco Uboldi ◽  
Andrea Gazzaniga ◽  
Lucia Zema ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Polyethylene Glycol ◽  
Injection Molding ◽  
Molar Mass ◽  
Oral Drug Delivery ◽  
Hydroxypropyl Methylcellulose ◽  
Oral Drug ◽  
Mechanical Resistance ◽  
Molding Process ◽  
Functional Coating

Capsular devices for oral drug delivery were recently proposed and manufactured by injection molding (IM) as an evolution of traditional reservoir systems comprising a core and a functional coating. IM allowed the fabrication of capsule shells with release-controlling features based on the employed materials and the design characteristics. These features are independent of the drug, with significant savings in development time and costs. In previous work, IM was used to produce enteric-soluble capsules from blends of hydroxypropyl methylcellulose acetate succinate, with polyethylene glycol (PEG) as the plasticizer. In this work, the range of plasticizer concentrations and molar mass was broadened to evaluate in-depth how those parameters affect material processability and capsule performance over time. As expected, increasing the amount of the low molar mass plasticizer decreased the viscosity and modulus of the material. This simplified the molding process and enhanced the mechanical resistance of the shell, as observed during assembly. However, some samples turned out translucent, depending on several factors including storage conditions. This was attributed to plasticizer migration issues. Such results indicate that higher molar mass PEGs, while not significantly impacting on processability, lead to capsular devices with consistent performance in the investigated time lapse.

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