scholarly journals Chitosan-Coated 5-Fluorouracil Incorporated Emulsions as Transdermal Drug Delivery Matrices

Polymers ◽  
2021 ◽  
Vol 13 (19) ◽  
pp. 3345
Author(s):  
Taif Ali Khan ◽  
Abul Kalam Azad ◽  
Shivkanya Fuloria ◽  
Asif Nawaz ◽  
Vetriselvan Subramaniyan ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Transdermal Drug Delivery ◽  
Skin Permeation ◽  
Tween 80 ◽  
Lauryl Sulfate ◽  
Good Penetration ◽  
Model Drug ◽  
Penetration Profile ◽  
Premature Release

The purpose of the present study was to develop emulsions encapsulated by chitosan on the outer surface of a nano droplet containing 5-fluorouracil (5-FU) as a model drug. The emulsions were characterized in terms of size, pH and viscosity and were evaluated for their physicochemical properties such as drug release and skin permeation in vitro. The emulsions containing tween 80 (T80), sodium lauryl sulfate, span 20, and a combination of polyethylene glycol (PEG) and T20 exhibited a release of 88%, 86%, 90% and 92%, respectively. Chitosan-modified emulsions considerably controlled the release of 5-FU compared to a 5-FU solution (p < 0.05). All the formulations enabled transportation of 5-FU through a rat’s skin. The combination (T80, PEG) formulation showed a good penetration profile. Different surfactants showed variable degrees of skin drug retention. The ATR-FTIR spectrograms revealed that the emulsions mainly affected the fluidization of lipids and proteins of the stratum corneum (SC) that lead to enhanced drug permeation and retention across the skin. The present study concludes that the emulsions containing a combination of surfactants (Tween) and a co-surfactant (PEG) exhibited the best penetration profile, prevented the premature release of drugs from the nano droplet, enhanced the permeation and the retention of the drug across the skin and had great potential for transdermal drug delivery. Therefore, chitosan-coated 5-FU emulsions represent an excellent possibility to deliver a model drug as a transdermal delivery system.

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 AND DEVELOPMENT OF TRANSDERMAL DRUG DELIVERY SYSTEM OF ETHINYLESTRADIOL AND TESTOSTERONE: IN VITRO EVALUATION

2019 ◽  
Vol 11 (1) ◽  
pp. 55
Author(s):  
Shikha Baghel Chauhan ◽  
Tanveer Naved ◽  
Nayyar Parvez
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Transdermal Drug Delivery ◽  
Skin Permeation ◽  
Physical Parameters ◽  
Transdermal Patch ◽  
Transdermal Drug Delivery System ◽  
In Vitro Skin Permeation

Objective: The combination therapy of ethinylestradiol and testosterone in post-menopausal females has shown improved sexual response and libido. The present studies were designed to develop a suitable matrix-type transdermal drug delivery system (TDDS) of ethinylestradiol and testosterone using the polymer chitosan.Methods: Five formulations (ET1 to ET5) were developed by varying the concentration of polymer and keeping the drug load constant. Physical parameters and drug excipient interaction studies were evaluated in all the formulations. In vitro skin permeation profiles of ethinylestradiol and testosterone from various formulations were simultaneously characterized in a thermostatically controlled modified Franz Diffusion cell using HPLC. Based on the physical parameters and in vitro skin permeation profile formulation ET3 containing 30 mg/ml of chitosan was found to be the best and chosen for further studies. Optimized formulation was subjected to in vivo pharmacokinetic analysis in rats using ELISA.Results: Stability profile of patch formulation ET3 depicted stability up to 3 mo. One week skin irritation evaluation in rats indicated that formulation ET3 was nonirritating. Combination transdermal patch across rat skin showed a maximum release of 92.936 and 95.03 % in 60 h with a flux of 2.088 and 21.398 µg/cm2h for ethinylestradiol and testosterone respectively.Conclusion: The net result of this study is the formulation of a stable, non-irritating transdermal patch of ethinylestradiol and testosterone, with good bioavailability and can be used as Estrogen Replacement Therapy (ERT) in postmenopausal women.

scholarly journals IN VITRO STUDY OF A TRANSFERSOMAL GEL PREPARATION CONTAINING LYNESTRENOL AS A TRANSDERMAL DRUG DELIVERY SYSTEM

2020 ◽  
pp. 242-244
Author(s):  
NURFITRIYANA NURFITRIYANA ◽  
HARMITA HARMITA ◽  
ISKANDARSYAH ISKANDARSYAH
Keyword(s):  
Drug Delivery ◽  
Transdermal Drug Delivery ◽  
In Vitro Study ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Rat Skin ◽  
Transdermal Drug Delivery System ◽  
Lipid Film ◽  
In Vitro Evaluation

Objective: Lynestrenol, a progestin hormone derivative, can suppress the productions of endogenous estrogen and progesterone hormones (ovaries)to prevent ovulation. In this study, lynestrenol was included in various transfersomal gel preparations for its transdermal delivery into fat (F)-andnon-fat (NF)-containing skin tissues.Methods: Lynestrenol transfersome vesicles were prepared by encapsulating the drug in varied concentrations of phosphatidylcholine and Tween80 using lipid film hydration method. Transfersomes were produced in the form of gel preparations at a dose of 0.15 mg/week and evaluated fortheir particle size, percentage of entrapment efficiency, and particle polydispersity. We performed in vitro evaluations of the formulation variants F0(lynestrenol gel control) and F1 and F2 (lynestrenol transfersome gels) with variations in their phosphatidylcholine and Tween 80 content. We thenperformed an in vitro evaluation using the Franz diffusion cell (FDC) method for 12 h using all three formulations on F and NF-containing rat skin.Results: The FDC results demonstrated that lynestrenol was deposited into fat tissue and increased concentrations of Tween 80 (edge activator)increased lynestrenol delivery into this tissue. In addition, the percentages of drug penetration from NF rat skin treated with F0, F1, and F2 gels were19.56%, 20.13%, and 20.56%, respectively, and those from F rat skin were 17.16%, 17.38%, and 17.50%, respectively.Conclusion: In vitro evaluation using the FDC method indicates that transdermal drug delivery through to fat tissues using transfersomes is apromising method for lynestrenol delivery.

Effect of Edge Activator on Characteristic and in Vitro Skin Permeation of Meloxicam Loaded in Elastic Liposomes

2011 ◽  
Vol 194-196 ◽  
pp. 537-540 ◽  
Author(s):  
Sureewan Duangjit ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat
Keyword(s):  
Drug Delivery ◽  
Transdermal Drug Delivery ◽  
Skin Permeation ◽  
Cetylpyridinium Chloride ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Transdermal Drug Delivery System ◽  
Scanning Calorimetry ◽  
In Vitro Skin Permeation

The aim of this study was to prepare and investigate the potential use of liposomes in the transdermal drug delivery of meloxicam (MX). The vesicles containing a constant amount of MX, phosphatidylcholine (PC), cholesterol (Chol) and cetylpyridinium chloride (CPC) (1:5:1:1 MX/PC/Chol/CPC molar ratio) to obtain liposomes. MX loaded liposomes were investigated for particle size, zeta potential, entrapment efficiency (%EE) and in vitro skin permeation. The results indicated that the liposomes were spherical in structure, 77 to 100 nm in size and charged. The %EE of MX in the vesicles ranged from 55 to 56%. The elastic liposomes consisting of MX/PC/Chol/CPC provided a significantly higher skin permeation of MX compared to the other formulations. Fourier Transform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC) analysis indicated that the application of liposomes may disrupt the stratum corneum lipid. Our research suggests that MX loaded elastic liposomes can be potentially used as a transdermal drug delivery system.

scholarly journals Fabrication of Alginate-Based O/W Nanoemulsions for Transdermal Drug Delivery of Lidocaine: Influence of the Oil Phase and Surfactant

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2556
Author(s):  
Omar Sarheed ◽  
Manar Dibi ◽  
Kanteti V. R. N. S. Ramesh ◽  
Markus Drechsler
Keyword(s):  
Drug Delivery ◽  
Local Anesthetic ◽  
Transdermal Drug Delivery ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Good Choice ◽  
System Composition ◽  
Oil In Water

Transdermal drug delivery of lidocaine is a good choice for local anesthetic delivery. Microemulsions have shown great effectiveness for the transdermal transport of lidocaine. Oil-in-water nanoemulsions are particularly suitable for encapsulation of lipophilic molecules because of their ability to form stable and transparent delivery systems with good skin permeation. However, fabrication of nanoemulsions containing lidocaine to provide an extended local anesthetic effect is challenging. Hence, the aim of this study was to address this issue by employing alginate-based o/w nanocarriers using nanoemulsion template that is prepared by combined approaches of ultrasound and phase inversion temperature (PIT). In this study, the influence of system composition such as oil type, oil and surfactant concentration on the particle size, in vitro release and skin permeation of lidocaine nanoemulsions was investigated. Structural characterization of lidocaine nanoemulsions as a function of water dilution was done using DSC. Nanoemulsions with small droplet diameters (d < 150 nm) were obtained as demonstrated by dynamic light scattering (DLS) and cryo-TEM. These nanoemulsions were also able to release 90% of their content within 24-h through PDMS and pig skin and able to the drug release over a 48-h. This extended-release profile is highly favorable in transdermal drug delivery and shows the great potential of this nanoemulsion as delivery system.

scholarly journals Characterization and In Vitro Skin Permeation of Meloxicam-Loaded Liposomes versus Transfersomes

2011 ◽  
Vol 2011 ◽  
pp. 1-9 ◽  
Author(s):  
Sureewan Duangjit ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat
Keyword(s):  
Drug Delivery ◽  
Transdermal Drug Delivery ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Transdermal Drug Delivery System ◽  
Scanning Calorimetry ◽  
Stratum Corneum Lipid ◽  
In Vitro Skin Permeation ◽  
Ft Ir

The goal of this study was to develop and evaluate the potential use of liposome and transfersome vesicles in the transdermal drug delivery of meloxicam (MX). MX-loaded vesicles were prepared and evaluated for particle size, zeta potential, entrapment efficiency (%EE), loading efficiency, stability, and in vitro skin permeation. The vesicles were spherical in structure, 90 to 140 nm in size, and negatively charged ( to  mV). The %EE of MX in the vesicles ranged from 40 to 70%. Transfersomes provided a significantly higher skin permeation of MX compared to liposomes. Fourier Transform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC) analysis indicated that the application of transfersomes significantly disrupted the stratum corneum lipid. Our research suggests that MX-loaded transfersomes can be potentially used as a transdermal drug delivery system.

Investigating Non-Therapeutic Pharmaceutical Substances for Improving In-Vitro Efficacy of Clindamycin Phosphate Against MRSA and Staphylococcus Epidermidis

2020 ◽  
Vol 18 (2) ◽  
pp. 63-72
Author(s):  
Mohd Aftab Alam ◽  
Fahad I. Al-Jenoobi ◽  
Khaled A. Alzahrani ◽  
Mohammad H. Al-Agamy ◽  
Abdullah M. Al-Mohizea
Keyword(s):  
Fusidic Acid ◽  
Staphylococcus Epidermidis ◽  
Sorbic Acid ◽  
Tween 80 ◽  
Lauryl Sulfate ◽  
Individual Substance ◽  
Dependent Effect ◽  
Pharmaceutical Excipients ◽  
Active Substances

The aim of present study was to investigate the effect of pharmaceutical excipients and other active substances on antimicrobial efficacy of standard antibiotic against resistant and susceptible microorganisms. Pharmaceutical excipients (sodium lauryl sulfate [SLS], Tween-80, citric acid, NaOH, NaCl) and active substances (fusidic acid, sorbic acid) were investigated to check in-vitro efficacy and their effect on the efficacy of standard antibiotic. Clindamycin was selected as standard antibiotic. Clindamycin was found to be ineffective against methicillin-resistant Staphylococcus aureus (MRSA). Fusidic acid and SLS showed concentration dependent effect against MRSA. Other tested substances were also ineffective against MRSA, and also failed to improve the susceptibility of MRSA towards clindamycin. The clindamycin + fusidic acid (0.05 µg, 0.1 µg), and clindamycin + SLS (0.5 mg, 1 mg) showed concentration dependent effect on Staphylococcus epidermidis (S. epidermidis). Clindamycin combinations with fusidic acid or SLS showed better inhibition of S. epidermidis, than individual substance. At lower concentration of clindamycin (2 µg), the sorbic acid (25 µg) improves its effectiveness. SLS (0.5 mg, 1 mg) and clindamycin (4 µg, 10 µg) showed almost equal zone of inhibition against S. epidermidis, respectively. Present findings showed that certain pharmaceutical excipients (e.g. SLS) are effective against resistant and susceptible microbes, and suggested that more excipients should be screened for their antimicrobial potential and their ability to improve the efficacy of standard antibiotics.

scholarly journals COMPARATIVE EVALUATION OF SELECTED POLYMERS AND PLASTICIZER ON TRANSDERMAL DRUG DELIVERY SYSTEM

2018 ◽  
Vol 10 (1) ◽  
pp. 67
Author(s):  
Bhawana Sethi ◽  
Rupa Mazumder
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Propylene Glycol ◽  
Drug Delivery System ◽  
Transdermal Drug Delivery ◽  
Release Kinetics ◽  
Content Uniformity ◽  
Transdermal Drug Delivery System ◽  
Transdermal Patches

Objective: The present work was aimed at preparation of transdermal patches by a solvent casting method using a varying concentration of polymers i.e. methocel (K15 and K100), ethocel (4 and 10), gelatin, chitosan, eudragit (RL and RS) grade using plasticizer (glycerin and propylene glycol).Methods: The ratio of drug to polymers and plasticizer was varied and the effect of formulation variables was studied. Prepared transdermal patches were evaluated for physicochemical properties, in-vitro permeation studies, content uniformity, primary skin irritation studies and FT-IR studies.Results: The formulated transdermal patch by using Methocel K 100 M showed good physical properties. The average weight of patches prepared using glycerin as a plasticizer were ranged from 42.33-67.00 mg and propylene glycol as a plasticizer were ranged from 40.67-67.67 mg. The percentage moisture absorption varies from 1.76 to 10.73 for patches formulated using glycerin and 2.28 to 7.97 for propylene glycol patches. The percentage moisture loss from patches prepared using glycerin was ranged from 2.75 to 11.54 and 2.87 to 12.02 from propylene glycol. The water vapour transmission rate from patches prepared using glycerin was ranged from 0.25 to 0.92 and 0.41 to 1.76. The formulated patch showed the acceptable quantity of medicament ranged from (100.20-101.05%). This result met the test content uniformity as per BP (85% to 115%). According to that, the drug was consistent throughout the patches. The formulation PGD is considered as the best formulation, since it shows a maximum in vitro drug release as 43.75 % at 24 h. The drug release kinetics studied showed that the majority of formulations was following zero order.Conclusion: In conclusion, controlled release transdermal drug delivery system patches of aliskiren can be prepared using polymer combinations, with a different plasticizer. The release rate of drug depends upon the polymer. However, release kinetics followed zero order.

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