Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin 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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Formulation, Preparation, Characterization, and Evaluation of Dicarboxylic Ionic Liquid Donepezil Transdermal Patches

Pharmaceutics ◽

10.3390/pharmaceutics14010205 ◽

2022 ◽

Vol 14 (1) ◽

pp. 205

Author(s):

Linh Dinh ◽

Soohun Lee ◽

Sharif Md Abuzar ◽

Heejun Park ◽

Sung-Joo Hwang

Keyword(s):

Ionic Liquid ◽

Ex Vivo ◽

Optical Microscope ◽

Skin Permeability ◽

Resonance Spectroscopy ◽

Scanning Calorimetry ◽

Ionic Bonds ◽

Gastrointestinal Side Effects ◽

Permeability Studies

Donepezil (DPZ) is generally administered orally to treat Alzheimer’s disease (AD). However, oral administration can cause gastrointestinal side effects. Therefore, to enhance compliance, a new way to deliver DPZ from transdermal patch was developed. Ionic bonds were created by dissolving dicarboxylic acid and DPZ in ethanol, resulting in a stable ionic liquid (IL) state. The synthesized ILs were characterized by differential scanning calorimetry, optical microscope, Fourier transform infrared spectroscopy and nuclear magnetic resonance spectroscopy. The DPZ ILs were then transformed to a suitable drug-in-adhesive patch for transdermal delivery of DPZ. The novel DPZ ILs patch inhibits crystallization of the IL, indicating coherent design. Moreover, DPZ ILs and DPZ IL patch formulations performed excellent skin permeability compared to that of the DPZ free-base patch in both in vitro and ex vivo skin permeability studies.

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Solid lipid nanocarriers embedded hydrogel for topical delivery of apremilast: in-vitro, ex-vivo, dermatopharmacokinetic and anti-psoriatic evaluation

Journal of Drug Delivery Science and Technology ◽

10.1016/j.jddst.2021.102442 ◽

2021 ◽

pp. 102442

Author(s):

Vamshi Krishna Rapalli ◽

Swati Sharma ◽

Aniruddha Roy ◽

Amit Alexander ◽

Gautam Singhvi

Keyword(s):

Ex Vivo ◽

Topical Delivery ◽

Solid Lipid ◽

Lipid Nanocarriers

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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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Sodium alginate nanoparticles as a new transdermal vehicle of glucosamine sulfate for treatment of osteoarthritis

European Journal of Nanomedicine ◽

10.1515/ejnm-2017-0008 ◽

2017 ◽

Vol 9 (3-4) ◽

Cited By ~ 2

Author(s):

Asmaa S. El-Houssiny ◽

Azza A. Ward ◽

Dina M. Mostafa ◽

Salwa L. Abd-El-Messieh ◽

Kamal N. Abdel-Nour ◽

...

Keyword(s):

Side Effects ◽

Surface Charge ◽

Ex Vivo ◽

In Vitro Release ◽

Glucosamine Sulfate ◽

Suspension Stability ◽

Rat Skin ◽

Release Studies ◽

Vitro Release

AbstractGlucosamine sulfate (GS) has been used orally for the treatment of osteoarthritis (OA). However, it may be susceptible to the liver first pass phenomenon, which greatly affects its bioavailability, in addition to its side effects on the gastrointestinal tract. Alginate nanoparticles (Alg NPs) were investigated as a new drug carrier for transdermal delivery of GS to improve its effectiveness and reduce side effects. GS-Alg NPs were characterized by encapsulation efficiency, NP yield, particle size and surface charge properties. The in vitro release studies of GS and the ex vivo permeability through rat skin were determined using a UV-Vis spectrophotometer. GS-Alg NPs are within the nanometer range of size. High negative surface charge values are obtained and indicate the high suspension stability of the prepared formulation. The in vitro release studies showed that GS is released from Alg NPs in a sustained and prolonged manner. The ex vivo permeability of GS through rat skin is enhanced significantly after encapsulation in the negatively charged Alg NPs. We successfully reported a highly stable nanoparticlulate system using Alg NPs that permits the encapsulation of GS for topical administration, overcoming the disadvantages of oral administration.

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In Vivo and ex Vivo Approaches to Studying the Biomechanical Properties of Healing Wounds in Rat Skin

Journal of Biomechanical Engineering ◽

10.1115/1.4025109 ◽

2013 ◽

Vol 135 (10) ◽

Cited By ~ 14

Author(s):

Clare Y. L. Chao ◽

Gabriel Y. F. Ng ◽

Kwok-Kuen Cheung ◽

Yong-Ping Zheng ◽

Li-Ke Wang ◽

...

Keyword(s):

Wound Healing ◽

Ex Vivo ◽

Normal Skin ◽

Biomechanical Properties ◽

Skin Wound ◽

Sprague Dawley ◽

Rat Skin ◽

Mechanical Stiffness ◽

Air Jet

An evaluation of wound mechanics is crucial in reflecting the wound healing status. The present study examined the biomechanical properties of healing rat skin wounds in vivo and ex vivo. Thirty male Sprague-Dawley rats, each with a 6 mm full-thickness circular punch biopsied wound at both posterior hind limbs were used. The mechanical stiffness at both the central and margins of the wound was measured repeatedly in five rats over the same wound sites to monitor the longitudinal changes over time of before wounding, and on days 0, 3, 7, 10, 14, and 21 after wounding in vivo by using an optical coherence tomography-based air-jet indentation system. Five rats were euthanized at each time point, and the biomechanical properties of the wound tissues were assessed ex vivo using a tensiometer. At the central wound bed region, the stiffness measured by the air-jet system increased significantly from day 0 (17.2%), peaked at day 7 (208.3%), and then decreased progressively until day 21 (40.2%) as compared with baseline prewounding status. The biomechanical parameters of the skin wound samples measured by the tensiometer showed a marked reduction upon wounding, then increased with time (all p < 0.05). On day 21, the ultimate tensile strength of the skin wound tissue approached 50% of the normal skin; while the stiffness of tissue recovered at a faster rate, reaching 97% of its prewounded state. Our results suggested that it took less time for healing wound tissues to recover their stiffness than their maximal strength in rat skin. The stiffness of wound tissues measured by air-jet could be an indicator for monitoring wound healing and contraction.

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