scholarly journals Enhanced Skin Permeation of Estradiol by Dimethyl Sulfoxide Containing Transdermal Patches

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 320
Author(s):  
Anna Otterbach ◽  
Alf Lamprecht
Keyword(s):  
Dimethyl Sulfoxide ◽  
Model Compound ◽  
Storage Stability ◽  
Skin Permeation ◽  
Negative Control ◽  
Additional Benefit ◽  
Porcine Skin ◽  
Dermal Penetration ◽  
Transdermal Patches ◽  
Drying Conditions

Dimethyl sulfoxide is a well-known and widely used dermal penetration enhancer. Its incorporation in transdermal patches would be highly desirable; however, due to its volatility this is extremely challenging. Here, we report on the feasibility of a dimethyl sulfoxide (DMSO) containing transdermal system containing estradiol as a model compound. Transdermal patches were prepared from duro-tak® 387-2510 containing various DMSO concentrations at different drying temperatures. The resulting patches were analyzed for DMSO content, estradiol and DMSO release, estradiol and DMSO permeation through excised porcine skin, and recrystallization during stability testing. Drying conditions in the range of 35° to 40° allowed a complete polymer solvents removal while retaining significant amounts of DMSO (≤10 mg/patch). Estradiol skin permeation increased 4-fold (Jss = 4.12 µg/cm−2·h−1) compared to DMSO-negative control (Jss = 1.1 ± 0.2 µg/cm−2·h−1). As additional benefit, estradiol recrystallization was inhibited by DMSO at even lowest solvent concentrations. Storage stability was limited to 6 months at 25 °C with a surprising discrepancy between DMSO content (significantly lower) and flux (not significantly different). Although the technical feasibility range is relatively narrow, such DMSO-containing matrix-type patches are able to significantly enhance drug permeation through the skin while ameliorating the product stability against recrystallization.

scholarly journals An Investigation of the Influence of PEG 400 and PEG-6-Caprylic/Capric Glycerides on Dermal Delivery of Niacinamide

Polymers ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 2907
Author(s):  
Yanling Zhang ◽  
Majella E. Lane ◽  
David J. Moore
Keyword(s):  
Skin Permeation ◽  
Ternary Systems ◽  
Pharmaceutical Products ◽  
Porcine Skin ◽  
Peg 400 ◽  
Skin Delivery ◽  
Dermal Delivery ◽  
Binary And Ternary Systems ◽  
Skin Retention

Polyethylene glycols (PEGs) and PEG derivatives are used in a range of cosmetic and pharmaceutical products. However, few studies have investigated the influence of PEGs and their related derivatives on skin permeation, especially when combined with other solvents. Previously, we reported niacinamide (NIA) skin permeation from a range of neat solvents including propylene glycol (PG), Transcutol® P (TC), dimethyl isosorbide (DMI), PEG 400 and PEG 600. In the present work, binary and ternary systems composed of PEGs or PEG derivatives combined with other solvents were investigated for skin delivery of NIA. In vitro finite dose studies were conducted (5 μL/cm2) in porcine skin over 24 h. Higher skin permeation of NIA was observed for all vehicles compared to PEG 400. However, overall permeation for the binary and ternary systems was comparatively low compared with results for PG, TC and DMI. Interestingly, values for percentage skin retention of NIA for PEG 400:DMI and PEG 400:TC were significantly higher than values for DMI, TC and PG (p < 0.05). The findings suggest that PEG 400 may be a useful component of formulations for the delivery of actives to the skin rather than through the skin. Future studies will expand the range of vehicles investigated and also look at skin absorption and residence time of PEG 400 compared to other solvents.

scholarly journals FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF METOPROLOL TARTRATE USING PERMEATION ENHANCERS OF NATURAL AND SYNTHETIC ORIGIN

2019 ◽  
pp. 317-323
Author(s):  
SHIKHA BAGHEL CHAUHAN ◽  
SUSHILA SAINI
Keyword(s):  
Moisture Absorption ◽  
Skin Permeation ◽  
Penetration Enhancers ◽  
Moisture Loss ◽  
Metoprolol Tartrate ◽  
Peg 400 ◽  
Transdermal Patches ◽  
Weight Variation ◽  
Basil Oil

Objective: Oral metoprolol tartrate has a short elimination half-life (2-3h) and low bioavailability undergoes extensive first-pass metabolism and frequent dosing. The aim of the present investigation was to formulate, develop and evaluate metoprolol tartrate transdermal patches using various synthetic and natural penetration enhancers. Methods: Enhancers used were eugenol, limonene, basil oil, urea and SLS (sodium lauryl sulphate). Polymer used was chitosan and PEG 400 used as a plasticizer. Transdermal Films were prepared by using solvent casting method. FTIR and DSC were studied to assess any interaction between the drug and polymers. Films were evaluated for Physico-chemical Characteristics like thickness, weight variation, folding endurance, moisture loss, moisture absorption and drug content. In vitro skin permeation studies were performed using Keshary chien cell For 24 h across rat skin. Results: Chitosan was found to be a suitable polymer for matrix formation. 3.5% w/w was used to optimize to formulate transdermal patches. 1.5% of total solution v/v lactic acid was used for dissolution of chitosan. 2.5%v/v of total solution PEG 400 was used to provide plasticity and smoothness to the patches. From the evaluation of patches formulation, F10 containing Basil oil as penetration enhancer in the concentration of 1.5% v/v was found to be best among all batches because of its consistent release rate For 24 h and extent of drug release was 85.20%. It can be concluded that naturally occurring volatile oils i.e., terpenes appear acceptable permeation enhancer and shows the best permeation across skin as indicated by high percutaneous enhancement ability. Conclusion: The developed transdermal patches are stable, non-irritating, and had increased efficacy of metoprolol and therefore had a good potential for hypertension treatment.

scholarly journals Odorless Glutathione Microneedle Patches for Skin Whitening

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 100
Author(s):  
Yechan Lee ◽  
Sujeet Kumar ◽  
Sou Hyun Kim ◽  
Keum-Yong Seong ◽  
Hyeseon Lee ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Reduced Glutathione ◽  
Skin Permeation ◽  
Oxygen Species ◽  
Porcine Skin ◽  
New Approach ◽  
Skin Whitening ◽  
Protein Thiols ◽  
Good Pattern ◽  
Foul Odor

Glutathione is a natural anti-aging substance that prevents the oxidation of protein thiols from reactive oxygen species. In the pharmaceutical industry, reduced glutathione (GSH) has been widely used for skin whitening due to its ability to inhibit tyrosinase. However, its poor permeability and foul odor limit its use in skin applications. Herein, we report a GSH-loaded dissolving microneedle (MN) patch prepared with hyaluronic acid (HA) that enables enhanced permeation across the skin and reduces the foul odor of GSH. HA was selected to prepare odorless GSH solutions and used for MN fabrications as a carrier of GSH. GSH-loaded MN (GSH-MN) arrays prepared from MN-forming solution containing up to 10% GSH showed good pattern uniformity and appropriate mechanical properties for insertion into the skin. The GSH-MNs with a loading capacity of 17.4% dissolve within 10 min following insertion into porcine skin and release the loaded GSH without being oxidized. This new approach combines functional biopolymers to reduce the characteristic GSH odor and advanced transdermal delivery based on MN technology to enhance skin permeation without pain. We believe this technique could expand the application of GSH in many cosmeceutical fields.

Design and Development of Propranolol Hydrochloride Transdermal Patches: In Vitro and Ex Vivo Characterization

2020 ◽  
Vol 3 (1) ◽  
pp. 01-08
Author(s):  
Chinthakindi Shravya
Keyword(s):  
Drug Release ◽  
Moisture Absorption ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Diffusion Mechanism ◽  
Propranolol Hydrochloride ◽  
Matrix Type ◽  
Transdermal Patches ◽  
Percent Moisture

The main aim of this investigation is to design and develop matrix type transdermal patches of Propranolol Hydrochloride which is an anti-hypertensive drug. These matrix type transdermal patches were prepared by “Solvent Casting Technique” using drug, HPMC E15 and Eudragit L 100 in the ratio of 1:6, 1:6.5, 1:7, 1:7.5, 1:8, 1:8.5, 1:9, 1:9.5. All formulations carried 20%v/w of PEG-600 as plasticizer. The prepared patches were characterized for various physicochemical parameters like weight, thickness, folding endurance, drug content, percent moisture content, percent moisture absorption, in vitro drug release and ex vivo permeation. Among this 1:9 ratio was found to be an Optimized formulation and patches were prepared by using permeation enhancers (lemon grass oil, Eucalyptus oil, and clove oil). The cumulative amount of drug release in 12hrs for F7 formulation showed maximum and used for that formulation skin permeation on Goat abdominal skin. FTIR studies show no interaction between drug, polymer and other excipients. The drug permeation kinetics followed “First order” and “zero order” profile with diffusion mechanism.

Development and Characterization of Gantrez® S-97 and Hyaluronic Acid Microneedles for Transdermal Fluorescein Sodium Delivery

2020 ◽  
Vol 859 ◽  
pp. 125-131 ◽  
Author(s):  
Phuvamin Suriyaamporn ◽  
Worranan Rangsimawong ◽  
Praneet Opanasopit ◽  
Tanasait Ngawhirunpat
Keyword(s):  
Drug Delivery ◽  
Hyaluronic Acid ◽  
Drug Delivery System ◽  
Delivery System ◽  
Transdermal Drug Delivery ◽  
Skin Permeation ◽  
Skin Permeability ◽  
Fluorescein Sodium ◽  
Porcine Skin ◽  
Transdermal Drug Delivery System

Microneedles (MNs) are attractive micron scale technology, which has been used as a physical force to create transport pathways and enhance the permeability of drugs into the skin. Fluorescein sodium (FS), a hydrophilic drug was loaded in MNs for transportation through skin. The purposes of this study were to develop and evaluate the optimal formulation of FS-loaded polymeric microneedles (MNs) as a device for transdermal drug delivery system. The FS-MNs were fabricated by micro-molding technique and prepared by using Gantrez® S-97 (G) and hyaluronic acid (HA). The physical appearances were observed under digital microscope. The mechanical properties were determined by a texture analyzer. The insertion study was tested on neonatal porcine skin. The MNs height changing after insertion into the skin at predetermined times was measured to show dissolution ability of MNs. Finally, the drug permeation profile of FS-MNs was investigated by Franz diffusion cell. For the results, all formulations were complete fabrication of conical microneedle array (11 rows x 11 columns in 10 mm2 patch area) with average 600 + 20 μm in height, 300 + 5 μm in width, and 600 + 10 μm in interspace. The percent decrease of MNs height in mechanical strength of 30%G+5%HA was significantly less than others at 1.8 to 8.8 N/121 array. The formulation mixing with 30% Gantrez® S-97 had 100% of penetration into porcine skin. The dissolution ability showed that MNs were completely dissolved within 60 minutes. At 24 h of skin permeation, the FS permeated through the skin from 1%FS solution, 30%G+1%FS MNs, and 30%G+5%HA+1%FS MNs was 1.00%, 4.27% and 7.53%, respectively. The flux values of 1%FS solution, 30%G+1%FS MNs, and 30%G+5%HA+1%FS MNs were 0.006 μg/cm2/min, 0.032 μg/cm2/min, and 0.037 μg/cm2/min, respectively, indicating the highest skin permeability of FS from 30%G+5%HA+1%FS MNs. In conclusion, the 30%G+5%HA+1%FS formulation presented appropriate MNs properties as a device for transdermal drug delivery system.

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