Nanocarriers and their Actions to Improve Skin Permeability and Transdermal Drug Delivery

Sonophoresis temporarily increases skin permeability such that medicine can be delivered transdermally. Cavitation is believed to be the predominant mechanism in sonophoresis. In this study, an ultrasound contrast agent (UCA) strategy was adopted instead of low frequency ultrasound to assure that cavitation occurred, and the efficacy of sonophoresis with UCA was quantitatively analyzed by optical measurements. The target drug used in this study was 0.1 % Definity® in 70% glycerol, which was delivered into porcine skin samples. Glycerol was used because it is an optical clearing agent, and the efficiency of glycerol delivery could be analyzed with optical measurements. The applied acoustic pressure was approximately 600 kPa at 1 MHz ultrasound with a 10% duty cycle for 60 minutes. Experimental results indicated that the measured relative contrast (RC) after sonophoresis with UCA was approximately 80% higher than RC after sonophoresis without UCA. In addition, the variance of RC was also reduced by more than 50% with the addition of a UCA. The use of a UCA appeared to increase cavitation, demonstrating that the use of a UCA can be effective in transdermal drug delivery (TDD).

Download Full-text

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

Key Engineering Materials ◽

10.4028/www.scientific.net/kem.859.125 ◽

2020 ◽

Vol 859 ◽

pp. 125-131 ◽

Cited By ~ 1

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.

Download Full-text

Skin permeability: Dermatologic aspects of transdermal drug delivery

American Heart Journal ◽

10.1016/0002-8703(84)90576-3 ◽

1984 ◽

Vol 108 (1) ◽

pp. 200-206 ◽

Cited By ~ 31

Author(s):

Albert M. Kligman

Keyword(s):

Drug Delivery ◽

Transdermal Drug Delivery ◽

Skin Permeability

Download Full-text

Combining Microbubble Contrast Agent with Pulsed-Laser Irradiation for Transdermal Drug Delivery

Pharmaceutics ◽

10.3390/pharmaceutics10040175 ◽

2018 ◽

Vol 10 (4) ◽

pp. 175 ◽

Cited By ~ 3

Author(s):

Ai-Ho Liao ◽

Ho-Chiao Chuang ◽

Bo-Ya Chang ◽

Wen-Chuan Kuo ◽

Chih-Hung Wang ◽

...

Keyword(s):

Drug Delivery ◽

Contrast Agent ◽

Transdermal Drug Delivery ◽

Ultrasound Contrast Agent ◽

Pulsed Laser ◽

Small Animal ◽

Skin Permeability ◽

Control Group

The optodynamic process of laser-induced microbubble (MB) cavitation in liquids is utilized in various medical applications. However, how incident laser radiation interacts with MBs as an ultrasound contrast agent is rarely estimated when the liquid already contains stable MBs. The present study investigated the efficacy of the laser-mediated cavitation of albumin-shelled MBs in enhancing transdermal drug delivery. Different types and conditions of laser-mediated inertial cavitation of MBs were first evaluated. A CO2 fractional pulsed laser was selected for combining with MBs in the in vitro and in vivo experiments. The in vitro skin penetration by β-arbutin after 2 h was 2 times greater in the group combining a laser with MBs than in the control group. In small-animal experiments, the whitening effect on the skin of C57BL/6J mice in the group combining a laser with MBs on the skin plus penetrating β-arbutin increased (significantly) by 48.0% at day 11 and 50.0% at day 14, and then tended to stabilize for the remainder of the 20-day experimental period. The present results indicate that combining a CO2 laser with albumin-shelled MBs can increase skin permeability so as to enhance the delivery of β-arbutin to inhibit melanogenesis in mice without damaging the skin.

Download Full-text

Optimizing Microneedle Arrays to Increase Skin Permeability for Transdermal Drug Delivery

Annals of the New York Academy of Sciences ◽

10.1111/j.1749-6632.2009.04083.x ◽

2009 ◽

Vol 1161 (1) ◽

pp. 83-94 ◽

Cited By ~ 48

Author(s):

Barrak Al-Qallaf ◽

Diganta Bhusan Das

Keyword(s):

Drug Delivery ◽

Transdermal Drug Delivery ◽

Skin Permeability ◽

Microneedle Arrays

Download Full-text

Skin hydration dynamics investigated by electrical impedance techniques in vivo and in vitro

Scientific Reports ◽

10.1038/s41598-020-73684-y ◽

2020 ◽

Vol 10 (1) ◽

Author(s):

Maxim Morin ◽

Tautgirdas Ruzgas ◽

Per Svedenhag ◽

Christopher D. Anderson ◽

Stig Ollmar ◽

...

Keyword(s):

Drug Delivery ◽

Transdermal Drug Delivery ◽

Electrical Impedance ◽

Skin Hydration ◽

Skin Impedance ◽

Skin Permeability ◽

Impedance Change ◽

Hydration Dynamics

Abstract Skin is easily accessible for transdermal drug delivery and also attractive for biomarker sampling. These applications are strongly influenced by hydration where elevated hydration generally leads to increased skin permeability. Thus, favorable transdermal delivery and extraction conditions can be easily obtained by exploiting elevated skin hydration. Here, we provide a detailed in vivo and in vitro investigation of the skin hydration dynamics using three techniques based on electrical impedance spectroscopy. Good correlation between in vivo and in vitro results is demonstrated, which implies that simple but realistic in vitro models can be used for further studies related to skin hydration (e.g., cosmetic testing). Importantly, the results show that hydration proceeds in two stages. Firstly, hydration between 5 and 10 min results in a drastic skin impedance change, which is interpreted as filling of superficial voids in skin with conducting electrolyte solution. Secondly, a subtle impedance change is observed over time, which is interpreted as leveling of the water gradient across skin leading to structural relaxation/changes of the macromolecular skin barrier components. With respect to transdermal drug delivery and extraction of biomarkers; 1 h of hydration is suggested to result in beneficial and stable conditions in terms of high skin permeability and extraction efficiency.

Download Full-text

DESIGN AND CHARACTERIZATION OF MICROEMULSION GEL FOR TRANSDERMAL DRUG DELIVERY SYSTEM OF DULOXETINE HYDROCHLORIDE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i11.27552 ◽

2018 ◽

Vol 11 (11) ◽

pp. 157

Author(s):

Karishma Tole ◽

Ganesh Deshmukh

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Transdermal Drug Delivery ◽

Tween 20 ◽

Skin Permeability ◽

Transdermal Drug Delivery System ◽

Method Optimization ◽

Stability Data ◽

Microemulsion Gel

Objective: The objective was to improve the bioavailability, stability of formulation, and skin permeability of Duloxetine HCl.Method: Microemulsion was prepared with oleic acid as oil, water, and Smix ratio of tween 20 to propylene glycol (1:3). Pseudo-ternary phase diagrams were constructed to determine the region of existence of microemulsions prepared using oil titration method. Optimization of formulations was done based on the in vitro diffusion studies. The microemulsion was gelled using carbopol 934p and HPMCK 100 as the gelling agent.Result: After the analysis of different evaluation parameter and drug release, the F3 batch was selected as a promising formulation for delivery of duloxetine HCl as a microemulsion gel for transdermal drug delivery with 79.607% drug release in 10 h.Conclusion: It was observed that transdermal microemulsion gel can be formulated successfully for duloxetine HCl with improved bioavailability. Among the other batches, the F3 batch was selected as an optimized batch because all the evaluation parameters results are satisfactory. From stability data, the formulation was found to be stable as no phase separation or turbidity was observed in the formulation after 3 months.

Download Full-text