Influence of Physicochemical Properties on the In Vitro Skin Permeation of the Enantiomers, Racemate, and Eutectics of Ibuprofen for Enhanced Transdermal Drug Delivery

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.

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

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.194-196.537 ◽

2011 ◽

Vol 194-196 ◽

pp. 537-540 ◽

Cited By ~ 7

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.

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

Journal of Drug Delivery ◽

10.1155/2011/418316 ◽

2011 ◽

Vol 2011 ◽

pp. 1-9 ◽

Cited By ~ 64

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.

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Effect of physicochemical properties of adhesive on the release, skin permeation and adhesiveness of adhesive-type transdermal drug delivery systems (a-TDD) containing silicone-based pressure-sensitive adhesives

International Journal of Pharmaceutics ◽

10.1016/0378-5173(91)90346-p ◽

1991 ◽

Vol 76 (1-2) ◽

pp. 77-89 ◽

Cited By ~ 12

Author(s):

R.D. Toddywala ◽

K. Ulman ◽

P. Walters ◽

Y.W. Chien

Keyword(s):

Drug Delivery ◽

Physicochemical Properties ◽

Transdermal Drug Delivery ◽

Drug Delivery Systems ◽

Skin Permeation ◽

Delivery Systems ◽

Pressure Sensitive Adhesives ◽

Pressure Sensitive ◽

Transdermal Drug Delivery Systems ◽

Adhesive Type

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

Polymers ◽

10.3390/polym13193345 ◽

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.

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Assessment of Finite and Infinite Dose In Vitro Experiments in Transdermal Drug Delivery

Pharmaceutics ◽

10.3390/pharmaceutics13030364 ◽

2021 ◽

Vol 13 (3) ◽

pp. 364

Author(s):

Luisa Coderch ◽

Ilaria Collini ◽

Victor Carrer ◽

Clara Barba ◽

Cristina Alonso

Keyword(s):

Drug Delivery ◽

Physicochemical Properties ◽

Transdermal Drug Delivery ◽

Diclofenac Sodium ◽

In Vitro Assays ◽

Pharmacokinetic Parameters ◽

Sodium Ibuprofen ◽

Pharmaceutical Industries ◽

Franz Diffusion Cells

Penetration, usually with finite dosing, provides data about the total active amount in the skin and permeation, being the most used methodology, usually with infinite dosing, leads to data about pharmacokinetic parameters. The main objective of this work is to assess if results from permeation, most of them at finite dose, may be equivalent to those from penetration usually at infinite dose. The transdermal behavior of four drugs with different physicochemical properties (diclofenac sodium, ibuprofen, lidocaine, and caffeine) was studied using penetration/finite and kinetic permeation/infinite dose systems using vertical Franz diffusion cells to determine the relationships between permeation and penetration profiles. Good correlation of these two in vitro assays is difficult to find; the influence of their dosage and the proportion of different ionized/unionized compounds due to the pH of the skin layers was demonstrated. Finite and infinite dose regimens have different applications in transdermal delivery. Each approach presents its own advantages and challenges. Pharmaceutical industries are not always clear about the method and the dose to use to determine transdermal drug delivery. Being aware that this study presents results for four actives with different physicochemical properties, it can be concluded that the permeation/infinite results could not be always extrapolated to those of penetration/finite. Differences in hydrophilicity and ionization of drugs can significantly influence the lack of equivalence between the two methodologies. Further investigations in this field are still needed to study the correlation of the two methodologies and the main properties of the drugs that should be taken into account.

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

Molecules ◽

10.3390/molecules26092556 ◽

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.

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