scholarly journals Transferosomes a New Transformation in Research: A Review

2021 ◽  
pp. 56-105
Author(s):  
Allam Sasikala
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Surfactant Concentration ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Hepatic Metabolism ◽  
Span 80 ◽  
Tween 60 ◽  
Span 60 ◽  
Transdermal Route

The drugs mostly present are available with less bioavailability  and the problem arises with less permeation or solubility  so extensive work is done to enhance these mechanisms. Not only that drugs should pass hepatic metabolism, Inorder to improve its bioavailability they are formulated as transferosomes which can improve the patient compliance by delivering the drug through the transdermal-route. Soya lecithin is used as a phospholipid whereas Tween 60, Tween 80, Span 60 and Span 80 are used as edge activators. These formulations usually showed more entrapment efficiency. The reason behind this is due to the presence of more phospholipids and as the surfactant concentration increases drug release will be rapid. As our main aim is to enhance the bioavailability this can be achieved by optimizing the concentrations of phospholipid and surfactant one can attain a controlled release of drug through this drug delivery system.

scholarly journals Formulation and Evaluation of Transferosomes Loaded with an Anti-Hyperlipidemic Drug

2021 ◽  
pp. 65-71
Author(s):  
R. Pravalika ◽  
E. Hima Bindu ◽  
V. T. Iswariya ◽  
Sowjanya Battu
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Surface Morphology ◽  
Drug Delivery System ◽  
Surfactant Concentration ◽  
Entrapment Efficiency ◽  
Hepatic Metabolism ◽  
Oral Route ◽  
Sem Analysis ◽  
Transdermal Route

The primary goal of this research is to create transferosome formulations that contain an anti-hyperlipidemic medication. Simvastatin, the medication employed in the formulation, has a low bioavailability of 60% and undergoes substantial hepatic degradation. These are the deformable nano-vesicles which can deliver both hydrophilic and hydrophobic drugs through transdermal route to enhance the Bioavailability of drugs which undergoes extensive hepatic metabolism when given through oral route which can increase patient compliance. Transferosomes are prepared and characterized by various evaluation tests like  SEM analysis, vesicular size,  surface morphology. After all evaluations done,  Out of 12 formulations F2 formulation showed more entrapment efficiency. The reason for this is that there are more phospholipids present, and as the surfactant concentration rises, medication release becomes more rapid. Our main goal is to improve bioavailability, which can be accomplished by optimising the concentrations of phospholipid and surfactant in this drug delivery system, resulting in a controlled release of drug.

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.

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

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.

scholarly journals Formulation and Evaluation of Mupirocin Nimosomal Gel for Topical Drug Delivery System

2020 ◽  
Vol 13 (2) ◽  
pp. 7-17
Author(s):  
Rajesh Akki ◽  
Munagala Gayatri Ramya ◽  
K Navyasri ◽  
Singaram Kathirvel
Keyword(s):  
Drug Release ◽  
Evaluation Studies ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Drug Uptake ◽  
Ph Gradient ◽  
Release Studies ◽  
Uptake Process ◽  
Span 80 ◽  
Niosomal Gel

The present study was to formulate and evaluate the mupirocin niosomal gel using surfactants span 80 & tween 80 for the preparation of niosomes. Mupirocin entrapped niosomes were prepared by ether injection method and transmembrane pH gradient drug uptake process. Niosomes were prepared by altering the ratios between various non-ionic surfactants (span 80 & tween 80) whereas the concentration of cholesterol and drug was kept constant. The prepared niosomes were characterized for size, shape, entrapment efficiency, invitro drug release studies. The highest entrapment efficiency(99.17%) and drug release (96.14%) was obtained for tween 80 (1:5:5) prepared by transmembrane pH gradient method. The best formulation among the two techniques was selected for incorporated into gel formulation. The prepared niosomal gel and plain gel were subjected to evaluation studies like drug content, invitro drug diffusion studies. The studies were demonstrated that niosomal gel was shown beter pharmacological activity than the conventional mupirocin gel. Based on the results it was concluded that niosomal preparations offers more advantageous than the conventional preparations.

Formulation, Development and Characterization of Floating Beads of Diltiazem Hydrochloride

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Anamika Saxena Saxena ◽  
Santosh Kitawat ◽  
Kalpesh Gaur ◽  
Virendra Singh
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Entrapment Efficiency ◽  
Repeated Administration ◽  
Alginate Beads ◽  
Delivery Systems ◽  
Sem Analysis ◽  
Formulation Development

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and nontoxic for a prolonged period. Various attempts have been made to develop gastroretentive delivery systems such as high density system, swelling, floating system. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration. Due to repeated administration there may be chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability and better patient compliance. Methodology: Five formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared. Alginate beads were prepared by ionotropic external gelation technique using CaCl2 as cross linking agent. Prepared beads were evaluated for % yield, entrapment efficiency, swelling index in 0.1N HCL, drug release study and SEM analysis. In order to improve %EE and drug release, LMP and sunflower oil were used as copolymers along with sodium alginate.

scholarly journals Formulation, characterization, evaluation and in vitro study of transfersomal gel medroxyprogesterone acetate for transdermal drug delivery

2020 ◽  
Vol 11 (4) ◽  
pp. 5373-5381
Author(s):  
Iskandarsyah ◽  
Camelia Dwi Putri Masrijal ◽  
Harmita
Keyword(s):  
Drug Delivery ◽  
Medroxyprogesterone Acetate ◽  
Transdermal Drug Delivery ◽  
High Performance ◽  
Hormonal Contraception ◽  
In Vitro Study ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Reversed Phase

A hormonal contraception progestin such as medroxyprogesterone acetate (MPA) is used to helps regulate ovulation thus as a part of contraception hormone therapy as a method of birth control. This study aimed to formulate, characterized, evaluated transfersomal gel containing medroxyprogesterone acetate and to increased subcutaneous penetration of medroxyprogesterone acetate. In this research, three transfersomes formulas were prepared and optimized, e.g. F1, F2 and F3 with phosphatidylcholine: tween 80 concentration were 90:10; 85:15; and 75:25, respectively. F2 was the best formula with the highest entrapment efficiency 81.20±0.42 %, Average 81.35 ±0.78 nm, morphology of vesicles were spheres, indeks polidispersity 0.198±0.012 and zeta potential was -34.83±0.64 mV. The transpersonal gel (FGT) containing F2, and non-transpersonal gel containing MPA in methanol(FG) were prepared. In vitro penetration test were conducted to both of them using Franz Diffusion cells. Analysis of medroxyprogesterone acetate used a high performance liquid chromatographic (HPLC) method with an ultraviolet detector on reversed-phase C18, 5µm; 150 x 4.6 mmcolumn; using acetonitrile-0.1% formic acid (60:40/v:v) and was detected at a wavelength of 240 nm with flow rate at 1.0 mL/min. Gel stability evaluation results showed that FGT was better than FG on pH stability, viscosity and rheological properties. Based on in vitro penetration study, cumulative subcutaneous penetration of medroxyprogesterone acetate from FGT was 2356.45 ± 197.73 ng.cm-2 and from FG 359.15 ± 13.60 ng.cm-2, respectively. Flux value for FGT and FG were 112.77 ± 6,47 ng.cm-2.hr-1and 17.99 ± 4.81 ng.cm-2.hr-1, respectively. It could be concluded that transfersomal gel medroxyprogesterone acetate for transdermal drug delivery increased cumulative transdermal penetration of medroxyprogesterone acetate by six times more than non-transfersomal gel dosage form.

scholarly journals FORMULATION, OPTIMIZATION AND IN VITRO EVALUATION OF 5-FLUOROURACIL LOADED LIQUORICE CRUDE PROTEIN NANOPARTICLES FOR SUSTAINED DRUG DELIVERY USING BOX-BEHNKEN DESIGN

2021 ◽  
pp. 216-226
Author(s):  
GEETHA V. S. ◽  
MALARKODI VELRAJ
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Crude Protein ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Sustained Drug Delivery ◽  
Drug Loading Efficiency

Objective: To formulate, optimize and evaluate 5-fluorouracil loaded liquorice crude protein nanoparticles for sustained drug delivery using Box-Behnken design. Methods: 5-fluorouracil (5-FU) loaded liquorice crude protein (LCP) nanoparticles were prepared by desolvation method using ethanol-water (1:2 ratio), Tween-80 (2%v/v) as stabilizing agent and gluteraldehyde (8% v/v) as cross linking agent. The optimization of prepared nanoparticles was carried out using Box-Behnken design with 3 factors 2 levels and 3 responses. The independent variables were A)5-FU concentration B)LCP concentration and C) sonication time while the responses were R1) Drug entrapment efficiency R2) Drug loading efficiency and R3) Particle size. The correlation between factors and responses were studied through response surface plots and mathematical equations. The nanoparticles were evaluated for FTIR, physicochemical properties like particle size and zeta potential by Photon correlation spectroscopy (PCS) and surface morphology by TEM. The entrapment efficiency, drug loading efficiency and in vitro drug release studies in PBS pH 7.4 (24 h) were carried out. The observed values were found to be in close agreement with the predicted value obtained from the optimization process. Results: 5-fluorouracil loaded LCP nanoparticles were prepared by desolvation method, the optimization was carried out by Box-Behnken design and the final formulation was evaluated for particle size (301.1 nm), zeta-potential (-25.8mV), PDI(0.226), with entrapment efficiency (64.07%), drug loading efficiency (28.54%), in vitro drug release (65.2% in 24 h) respectively. The formulated nanoparticles show Higuchi model drug release kinetics with sustained drug delivery for 24 h in pH7.4 buffer. Conclusion: The results were proved to be the most valuable for the sustained delivery of 5-Fluorouracil using liquorice crude protein as carrier. 5-FU–LCP nanoparticles were prepared using Tween-80 as stabilizing agent and gluteraldehyde as cross-linking agent to possess ideal sustained drug release characteristics.

scholarly journals BI-GELS: A NOVEL MATERIAL FOR TRANSDERMAL DRUG DELIVERY

2021 ◽  
pp. 1-5
Author(s):  
SARIPILLI RAJESWARI ◽  
RAJESWARI PULLABHATLA ◽  
CHUKKA YERNI SATYAVATHI
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Transdermal Drug Delivery ◽  
Drug Release Rate ◽  
Drug Delivery Vehicles ◽  
Novel Material ◽  
Delivery Vehicles ◽  
Semi Solid ◽  
Transdermal Route ◽  
Application Property

Bi-gels semi solid formulation is combination of organogel and hydrogel with better application property such as pharmaceutical and cosmetics. The main objective of this review is specially focuses on application of bi-gels as drug delivery vehicles by transdermal route. It contains two different phases which are polar and nonpolar due to which, it possess some significant features such as ability to deliver the hydrophilic and hydrophobic drugs which also have improved permeability of drugs, better spreading ability, and water wash ability. Hence, bigels have both organogels and hydrogels they can enhanced hydration of stratum corneum and also had an ability to manipulate the drug release rate from the dosage from.

scholarly journals Effect of nonionic surfactants on the release of paracetamol from suppositories

2015 ◽  
Vol 26 (1) ◽  
pp. 40-44
Keyword(s):  
Drug Release ◽  
Physical Properties ◽  
Phosphate Buffer ◽  
Nonionic Surfactants ◽  
Tween 80 ◽  
Content Uniformity ◽  
Fusion Method ◽  
Disintegration Time ◽  
Span 60

The preparation suppositories contain 250 mg of paracetamol on different bases using Novata BD, Novata BCF and composition of Novata BCF/BD (1:1). Suppositories were prepared by the fusion method. The prepared formulations with or without surfactants (Tween 80, Span 60) at concentrations of 2% and 4% (w/w) were tested for hardness, to tal time of de for ma tion, disintegration time, content uniformity and release of the drug. The release of the drug was carried in the apparatus with the stirrer shade in phosphate buffer (pH 7.2) at 100 rpm. The physical properties of the prepared suppositories were according with the requirement of Polish Pharmacopoeia 9th edition. Addition of 4 % Tween 80 to suppository bases significantly increased the drug release from all the investigated formulations. However, incorporation of Span 60 did not result in improvement of the drug release significantly.

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

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