Improved skin permeability and whitening effect of catechin-loaded transfersomes through topical delivery

AbstractFungal infections have become a subject of great concern and the incidence of fungal infections is increasing, presenting an enormous challenge to healthcare professionals. Since most of the fungal infections are occurring over the skin, the treatment option of these infections always involves topical application. However, in topical delivery drug reaches into systemic circulation through different barriers of skin. Nevertheless, due to the low permeability, skin restricts the movement of many drugs. Hence, a delivery system is required, which deliver the medicament into the skin layers or through the skin and into the systemic circulation. Ethosomes or Soft malleable vesicles are the novel lipid vesicular carrier that offer improved skin permeability and efficient delivery due to their structure and composition. They contain high concentration of ethanol, which increases the fluidity of the skin. Therefore, in the present paper, we have explored the utility of ethosomal systems in the topical treatment of fungal infections. Structure, compositions types, mechanism and techniques of preparation of ethosome also discussed in the paper.

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Combination of Microemulsion for Topical Deliverying Tripterygium Wilfordii Multiglycoside

Materials Science Forum ◽

10.4028/www.scientific.net/msf.694.881 ◽

2011 ◽

Vol 694 ◽

pp. 881-885

Author(s):

Xin He ◽

Xing Hua Zhao ◽

Wu Qing Ou Yang

Keyword(s):

Immune Suppression ◽

Topical Delivery ◽

Skin Permeability ◽

Tripterygium Wilfordii ◽

Delivery Vehicle ◽

Control Solution ◽

Suppression Effect ◽

Low Viscosity ◽

Spherical Droplets

The purpose of this study was to explore the potential application of the combination of microemulsion as a topical delivery vehicle in enhancing the absorption and efficacy of tripterygium wilfordii multiglycoside (TWM). Various microemulsion formulations were developed and an optimal microemulsion (TWM-ME)，which presented spherical droplets and consisted of RH-40, IPM and water was 27: 3.3: 69.7 by weight. It possessd an average droplet size of 23.6 nm, a low viscosity of (3.56±0.12) mm2•s-1 Zeta electric potential was (–5.35±0.42) mV, refractive index was (1.3617±0.0051) nD20, conductivity was (97.6±3.6) μs/cm. Compared to the control solution, TWM-ME provided better skin permeability in vitro. Moreover, TWM-ME has noticeable anti-inflammatory and immune suppression effect. These results indicate that the combination of microemulsion represents an effective vehicle for topical delivery of TWM.

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NANOEMULSION GEL OF NUTRACEUTICAL CO-ENZYME Q10 AS AN ALTERNATIVE TO CONVENTIONAL TOPICAL DELIVERY SYSTEM TO ENHANCE SKIN PERMEABILITY AND ANTI-WRINKLE EFFICIENCY

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i11.21751 ◽

2017 ◽

Vol 9 (10) ◽

pp. 207

Author(s):

Eman S. El- Leithy ◽

Amna M. Makky ◽

Abeer M. Khattab ◽

Doaa G. Hussein

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Ex Vivo ◽

Topical Delivery ◽

Water Soluble ◽

Skin Permeability ◽

Isopropyl Myristate ◽

Promising Alternative ◽

Drug Content ◽

Nanoemulsion Gel

Objective: The object of our investigation was to develop and characterize nanoemulsion gel (NEG) as transdermal delivery systems for the poorly water soluble drug, Co-enzyme Q10 (CoQ10), to improve its solubility and skin permeability and thus improving its anti-wrinkle efficiency.Methods: An optimized nanoemulsion (NE) formula was chosen according to its particle size and stability and converted into nanoemulsion gel using different gelling agents, including; carbopol 934 (1%), xanthan gum (2%) and sodium carboxymethyl cellulose(NaCMC) (2%). Drug loaded nanoemulsion gels were characterized for particle size, zeta potential, viscosity and rheological behavior, conductivity, spreadability, drug content and permeation studies using Franz diffusion cell.Results: NEG containing 10% w/v isopropyl myristate (IPM) as oil, 60% w/v tween 80 and transcutol HP as surfactant/co-surfactant mixture (S/CoS), 30%w/v water, 2%w/v drug, and 1% w/v carbopol 934 as gelling gent was concluded as an optimized NEG formula. It exhibited pH, viscosity, drug content, particle size, zeta potential, polydispersity index(PDI) and spreadability, as 5.4±0.011, 27588±2034.34 cps,101.51±0.93%,120.5±1.19 nm,-29.8±1.46, 0.273 and 6.16±0.28 cm, respectively. Also, it showed significantly higher cumulative amount of drug permeated through dialysis membrane (281.71±0.97μg/cm2) and through rat skin (20.73±2.5 μg/cm2) than the other formulae and marketed formulation (P<0.001). In addition, its permeability parameters like drug flux (Jss), enhancement ratio (Er) and permeability coefficient (Kp) exhibited the highest values; 12.79µg/cm2/h, 95.92×10-4 cm2/h and 57.35, respectively for in vitro permeation study and 0.968µg/cm2/h, 7.26×10-4 cm2/h and 1.183, respectively for ex-vivo permeation study.Further histopathological evaluation test showed that CoQ10 NEG has a good anti-wrinkle efficacy compared to the conventional topical dosage form.Conclusion: These results judged NEG to be a promising alternative carrier for topical delivery of CoQ10 to enhance its solubility, skin permeability and thus anti-wrinkle efficiency.

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Nanoemulgel for Improved Topical Delivery of Retinyl Palmitate: Formulation Design and Stability Evaluation

Nanomaterials ◽

10.3390/nano10050848 ◽

2020 ◽

Vol 10 (5) ◽

pp. 848 ◽

Cited By ~ 4

Author(s):

Mohammed S. Algahtani ◽

Mohammad Zaki Ahmad ◽

Javed Ahmad

Keyword(s):

Droplet Size ◽

Delivery System ◽

Skin Irritation ◽

Topical Delivery ◽

Skin Aging ◽

Retinyl Palmitate ◽

Skin Permeability ◽

Therapeutic Benefits ◽

Behavior Study ◽

Hydrogel System

Retinyl palmitate is a vitamin A ester belonging to the family of endogenous natural retinoid and used to treat various skin disorders like acne, skin aging, wrinkles, and dark spots, as well as to protect against psoriasis. Despite the known therapeutic benefits of retinyl palmitate, the conventional topical delivery of retinyl palmitate commonly associated with adverse reactions such as skin irritation, redness, excessive peeling, and dryness. Therefore, the current study aims to encapsulate the retinyl palmitate in nanoemulsion then incorporate it into a hydrogel system to improve the topical delivery and stability. Low-energy emulsification method was used for the nano-encapsulation of retinyl palmitate. The phase behavior study was used for the investigation and the optimization of the formulation. The droplet size of the optimized nanoemulsion was in nano dimension (16.71 nm) with low polydispersity index (PdI) (0.015), negative zeta potential (−20.6 mV). It demonstrated the influence of vortexing on droplet size and PdI during nanoemulsion preparation. The retinyl palmitate loaded nanoemulgel delivery system exhibited significant improvement (p < 0.05) in skin permeability after topical application. Employment of the nano-encapsulation approach afterward dispersion into hydrogel system for the development of a topical delivery system of retinyl palmitate resulted in improvement in its UV and storage stability as well.

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Enhanced Skin Delivery of Therapeutic Peptides Using Spicule-Based Topical Delivery Systems

Pharmaceutics ◽

10.3390/pharmaceutics13122119 ◽

2021 ◽

Vol 13 (12) ◽

pp. 2119

Author(s):

Chi Zhang ◽

Jiwen Duan ◽

Yongxiang Huang ◽

Ming Chen

Keyword(s):

Blood Glucose ◽

Initial Level ◽

Topical Delivery ◽

Delivery Systems ◽

Marine Sponges ◽

Skin Permeability ◽

Skin Delivery ◽

Therapeutic Peptides

This study reports two therapeutic peptides, insulin (INS, as a hydrophilic model peptide) and cyclosporine A (CysA, as a hydrophobic one), that can be administrated through a transdermal or dermal route by using spicule-based topical delivery systems in vitro and in vivo. We obtained a series of spicules with different shapes and sizes from five kinds of marine sponges and found a good correlation between the skin permeability enhancement induced by these spicules and their aspect ratio L/D. In the case of INS, Sponge Haliclona sp. spicules (SHS) dramatically increased the transdermal flux of INS (457.0 ± 32.3 ng/cm2/h) compared to its passive penetration (5.0 ± 2.2 ng/cm2/h) in vitro. Further, SHS treatment slowly and gradually reduced blood glucose to 13.1 ± 6.3% of the initial level in 8 h, while subcutaneous injection resulted in a rapid blood glucose reduction to 15.9 ± 1.4% of the initial level in 4 h, followed by a rise back to 75.1 ± 24.0% of the initial level in 8 h. In the case of CysA, SHS in combination with ethosomes (SpEt) significantly (p < 0.05) increased the accumulation of CysA in viable epidermis compared to other groups. Further, SpEt reduced the epidermis thickness by 41.5 ± 9.4% in 7 days, which was significantly more effective than all other groups. Spicule-based topical delivery systems offer promising strategies for delivering therapeutic peptides via a transdermal or dermal route.

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Evaluation of Skin Permeability of Resveratrol Loaded Liposomes and Nanostructured Lipid Carriers using a Skin Mimic Artificial Membrane (skin-PAMPA)

Drug Delivery Letters ◽

10.2174/2210303109666190207152927 ◽

2019 ◽

Vol 9 (2) ◽

pp. 134-145 ◽

Cited By ~ 2

Author(s):

Marta Casamonti ◽

Vieri Piazzini ◽

Anna Rita Bilia ◽

Maria Camilla Bergonzi

Keyword(s):

Antioxidant Capacity ◽

In Vitro Release ◽

Topical Delivery ◽

Delivery Systems ◽

Nanostructured Lipid Carriers ◽

Skin Permeability ◽

Dpph Test ◽

Release Studies ◽

Vitro Release

Background: The skin-PAMPA test is a quick and relatively deep tool in the early stages of drug discovery and formulation of dermal and transdermal delivery systems. Objective: This study focused on the application of the skin-PAMPA test to evaluate the permeation of Resveratrol (RSV) and also of two formulations, Liposomes (LP) and Nanostructured Lipid Carriers (NLC), prepared to improve RSV topical delivery. Methods: LP and NLC were physically and chemically characterized. Stability and in vitro release studies were also assessed in different pH media. The release results were applied to define the kinetic and mechanism of RSV release from the LP and NLC formulations. In vitro permeability was estimated through the skin-PAMPA and the antioxidant capacity was evaluated by DPPH test. Results: Nanoparticles have a spherical shape, dimensions suitable for skin application, and narrow size distribution. Encapsulation efficiency was 96.5% ± 2.1 for LP and 86.0% ± 2.4 for NLC. The formulations increased RSV solubility. Nanoparticles showed excellent physical and chemical stability during storage at 4°C for two months. In vitro release studies were performed at pH 5.5 and 7.4. The nanoparticles achieved a prolonged release of RSV. Skin-PAMPA proved an increased cutaneous permeability of RSV when loaded into LP or NLC. Both formulations maintained the antioxidant capacity of RSV, as evidenced by DPPH test. Conclusion: LP and NLC could be applied as drug delivery systems suitable for the topical delivery of the RSV. Skin-PAMPA has proved to be an effective tool for studying the permeability not only of the RSV but also of its formulations.

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Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

Pharmaceutics ◽

10.3390/pharmaceutics12010025 ◽

2019 ◽

Vol 12 (1) ◽

pp. 25 ◽

Cited By ~ 4

Author(s):

Ayman Salama ◽

Mohamed Badran ◽

Mohammed Elmowafy ◽

Ghareb M. Soliman

Keyword(s):

Ex Vivo ◽

Topical Delivery ◽

Skin Permeability ◽

Sprague Dawley ◽

Rat Skin ◽

Dsc Studies ◽

Clinical Benefits ◽

Systemic Side Effects ◽

Permeability Studies

Spironolactone (SP), an aldosterone antagonist with anti-androgen properties, has shown promising results in the treatment of female acne. However, its systemic side effects limit its clinical benefits. This study aimed to prepare and evaluate LeciPlexes for SP topical delivery. LeciPlexes were prepared by a one-step procedure and characterized using various techniques. Optimum LeciPlex preparation was incorporated into 1% methylcellulose gel and SP permeability was tested ex vivo in Sprague-Dawley rat skin. The maximum drug encapsulation efficiency obtained was 93.6 ± 6.9% and was dependent on the drug/phospholipid and surfactant/phospholipid ratios. A zeta potential of +49.3 ± 3.5 to +57.7 ± 3.3 mV and a size of 108 ± 25.3 to 668.5 ± 120.3 nm were observed for the LeciPlexes. FT-IR and DSC studies confirmed the incorporation of SP into the LeciPlexes through hydrophobic and hydrogen bonding interactions. SP release from the LeciPlex formulations was significantly slower than from the drug suspension. Cumulative SP permeated through rat skin from LeciPlex gel was about 2-fold higher than SP control gel. Cumulative SP deposited in the stratum corneum and other skin layers from the LeciPlex gel was about 1.8- and 2.6-fold higher than SP control gel, respectively. This new SP LeciPlex formulation is a promising carrier for the treatment of female acne.

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Microsponges: An Overview

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v4i4.8860 ◽

2017 ◽

Vol 4 (4) ◽

Author(s):

Hamid Hussain ◽

Divya Juyal ◽

Archana Dhyani

Keyword(s):

Controlled Release ◽

Delivery System ◽

Oral Delivery ◽

Active Agent ◽

Topical Delivery ◽

Water Soluble ◽

Wide Range ◽

Porous Beads

Microsponge and Nanosponge delivery System was originally developed for topical delivery of drugs can also be used for controlled oral delivery of drugs using water soluble and bioerodible polymers. Microsponge delivery system (MDS) can entrap wide range of drugs and then release them onto the skin over a time by difussion mechanism to the skin. It is a unique technology for the controlled release of topical agents and consists of nano or micro porous beads loaded with active agent and also use for oral delivery of drugs using bioerodible polymers.

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