scholarly journals Enhancement of the Topical Bioavailability and Skin Whitening Effect of Genistein by Using Microemulsions as Drug Delivery Carriers

2021 ◽  
Vol 14 (12) ◽  
pp. 1233
Author(s):  
Quoc Lam Vu ◽  
Chih-Wun Fang ◽  
Muhammad Suhail ◽  
Pao-Chu Wu

Genistein, the most abundant isoflavone of the soy-derived phytoestrogen compounds, is a potent antioxidant and inhibitor of tyrosine kinase, which can inhibit UVB-induced skin carcinogenesis in hairless mice and UVB-induced erythema on human skin. In current study, genistein-loaded microemulsions were developed by using the various compositions of oil, surfactants, and co-surfactants and used as a drug delivery carrier to improve the solubility, peremability, skin whitening, and bioavailbility of genistein. The mean droplet size and polydispersity index of all formulations was less than 100 nm and 0.26 and demonstrated the formation of microemulsions. Similarly, various studies, such as permeation, drug skin deposition, pharmacokinetics, skin whitening test, skin irritation, and stability, were also conducted. The permeability of genistein was significantly affected by the composition of microemulsion formulation, particular surfactnat, and cosurfactant. In-vitro permeation study revealed that both permeation rate and deposition amount in skin were significantly increased from 0.27 μg/cm2·h up to 20.00 μg/cm2·h and 4.90 up to 53.52 μg/cm2, respectively. In in-vivo whitening test, the change in luminosity index (ΔL*), tended to decrease after topical application of genistein-loaded microemulsion. The bioavailability was increased 10-fold by topical administration of drug-loaded microemulsion. Conclusively, the prepared microemulsion has been enhanced the bioavailability of genistein and could be used for clinical purposes.

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 410
Author(s):  
Wan-Hsuan Hung ◽  
Ping-Kang Chen ◽  
Chih-Wun Fang ◽  
Ying-Chi Lin ◽  
Pao-Chu Wu

The aim of this study was to design oil in water (O/W) microemulsion formulations for the topical administration of azelaic acid. The permeability of azelaic acid through rat skin and the anti-inflammatory activities of the formulations were conducted to examine the efficacy of the designed formulations. Skin irritation and stability tests were also performed. The permeability of azelaic acid was significantly increased by using O/W microemulsions as carriers. The edema index of ear swelling percentage was significantly recovered by the 5% drug-loaded formulation and a 20% commercial product, demonstrating that the experimental formulation possessed comparable effect with the commercial product on the improvement of inflammation. The experimental formulation did not cause significant skin irritation compared to the negative control group. Moreover, the drug-loaded formulation also showed thermodynamic stability and chemical stability after storage for 30 days. In conclusion, the O/W microemulsion was a potential drug delivery carrier for azelaic acid topical application.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 163 ◽  
Author(s):  
Yongtai Zhang ◽  
Hongmei Hu ◽  
Qian Jing ◽  
Zhi Wang ◽  
Zehui He ◽  
...  

In the current study, diethylene glycol monoethyl ether-mediated microemulsions were combined with microneedles for enhanced transdermal aconitine delivery. The oil-in-water microemulsion increasedaconitine solubility and enhanced transdermal drug delivery and assistance with metal microneedles enhanced permeation of the aconitine-loaded microemulsion. Carried by the microemulsion, the in vitro permeability of aconitine was significantly enhanced, and further improved using microneedles. In vivo microdialysis revealed that the subcutaneous local drug concentration reached a high level within 30 min and remained relatively consistent to the end of the experimental period. AUC0-t of the microemulsion group was significantly higher than that of the aqueous solution group, and the microemulsion combined with microneedles group achieved the highest AUC0-t among the tested groups. The microemulsion and microdialysis probe also showed good biocompatibility with skin tissue. The microemulsion could be internalized by HaCaT and CCC-ESF-1 cells via lysosomes. The in vitro cytotoxicity of aconitine toward skin cells was reduced via encapsulation by microemulsion, and the prepared microemulsion developed no skin irritation. Hence, transdermal aconitine delivery and drug biosafety were effectively improved by loading into the microemulsion and assisting with microneedles, and in vivo microdialysis technique is suitable for realtime monitoring of transdermal drug delivery with microemulsion-based drug vehicles.


2020 ◽  
Vol 152 ◽  
pp. 105452
Author(s):  
Alexandra-Roxana Ilie ◽  
Brendan T. Griffin ◽  
Martin Brandl ◽  
Annette Bauer-Brandl ◽  
Ann-Christin Jacobsen ◽  
...  

Author(s):  
Om M Bagade ◽  
Shashikant N Dhole ◽  
Praveen D Chaudhar

Nanosponges have come into sight as one of the most promising fields of science because of their perceived applications in controlled drug delivery. It has been increasingly investigated to achieve targeted and sustained release of drugs. Nanosponges are one of the novel drug delivery system, which is gaining popularity now days because of their perceived application in controlled and site-specific drug delivery. The fundamental appeal of the nanosponge technology arises from the difficulty experienced with conventional formulations in releasing active ingredients over an extended period of time, unpleasant odor, greasiness and skin irritation. They are tiny sponge-like spherical particles with a large porous surface and are believed to contribute towards reduced side effects, improved stability, increased elegance and enhanced formulation flexibility. The present investigation in the appraisal describes nanosponge technology embracing its method of preparation, characterization, in-vitro and in-vivo evaluation methods along with recent research and future potential.


2014 ◽  
Vol 9 (2) ◽  
pp. 1934578X1400900
Author(s):  
Pedro Fong ◽  
Henry H. Y. Tong ◽  
Chi M. Chao

Although many herbal medicines are effective in the treatment of hyperpigmentation, the potency of different constituents remains unknown. In this work, more than 20,000 herbal ingredients from 453 herbs were docked into the crystal structures of adenylyl cyclase and a human homology tyrosinase model using Surflex-Dock. These two enzymes are responsible for melanin production and inhibition of them may attain a skin-whitening effect superior to currently available agents. The essential drug properties for topical formulation of the herbal ingredients, including skin permeability, sensitization, irritation, corrosive and carcinogenic properties were predicted by Dermwin, Skin Sensitization Alerts (SSA), Skin Irritation Corrosion Rules Estimation Tool (SICRET) and Benigni/Bossa rulebase module of Toxtree. Moreover, similarity ensemble and pharmacophore mapping approaches were used to forecast other potential targets for these herbal compounds by the software, SEArch and PharmMapper. Overall, this study predicted seven compounds to have advanced drug-like properties over the well-known effective tyrosinase inhibitors, arbutin and kojic acid. These seven compounds have the highest potential for further in vitro and in vivo investigation with the aim of developing safe and high-efficacy skin-whitening agents.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2129
Author(s):  
Elka Touitou ◽  
Hiba Natsheh

This review focuses on the improved topical treatment of various medical skin conditions by the use of drugs delivered from carriers containing phospholipid soft vesicles. Topical drug delivery has many advantages over other ways of administration, having increased patient compliance, avoiding the first-pass effect following oral drug administration or not requesting multiple doses administration. However, the skin barrier prevents the access of the applied drug, affecting its therapeutic activity. Carriers containing phospholipid soft vesicles are a new approach to enhance drug delivery into the skin and to improve the treatment outcome. These vesicles contain molecules that have the property to fluidize the phospholipid bilayers generating the soft vesicle and allowing it to penetrate into the deep skin layers. Ethosomes, glycerosomes and transethosomes are soft vesicles containing ethanol, glycerol or a mixture of ethanol and a surfactant, respectively. We review a large number of publications on the research carried out in vitro, in vivo in animal models and in humans in clinical studies, with compositions containing various active molecules for treatment of skin medical conditions including skin infections, skin inflammation, psoriasis, skin cancer, acne vulgaris, hair loss, psoriasis and skin aging.


2015 ◽  
Vol 1 (7) ◽  
pp. 300
Author(s):  
MAHENDRA PRASAD JATAV

AbstractArthritis is a disease of the joint that involves inflammation of one or more joints. The common symptoms of arthritis disorders include varied levels of pain, swelling, joint stiffness, and sometimes a constant ache around the joints. More than 20 million individuals with arthritis have severe limitations in function on a daily basis. The objective of this study was to resolve conventional dosage forms of NSAIDs, which are at increased risk for serious gastrointestinal complications, when administered through oral route. Topical administration of NSAIDs could deliver lornoxicam to the site of action in rheumatic diseases which would reduce the gastrointestinal complications and side effects of the drug. The prepared organogel of lornoxicam were evaluated for its appearance, organoleptic characteristic, viscosity, gelation temperature, drug content and in vitro release study. In vivo evaluation for analgesic activity of formulation was carried out in terms of skin irritation study, hot plate method, writhing test and edema paw induce method.Keywords- Lornoxicam, lecithin, organogel, Arthritis, Topical delivery.


2015 ◽  
Vol 3 (2) ◽  
pp. 267 ◽  
Author(s):  
Mahendra Prasad Jatav ◽  
Suman Ramteke

<p><strong>Background:</strong> Arthritis is a disease of the joint that involves inflammation of one or more joints. Topical administration of NSAIDs could deliver lornoxicam to the site of action in rheumatic diseases, which would reduce the gastrointestinal complications and side effects of the drug.</p><p><strong>Methods:</strong> In this method, the oily phase was prepared by dispersing the specific amount (ratio; 40:60) of purified lecithin at room temperature in isopropyl myristate as dispersing and emulsifying agent. The aqueous phase of polypropylene was prepared by dispersing a weighed amount of polypropylene and glycerol in water. It was stored at 2-4 oC overnight for the effective dissolution. The aqueous phase was slowly added in oily phase with stirring at 400 rpm using a mechanical stirrer. The prepared organogel of lornoxicam were evaluated for its appearance, organoleptic characteristic, viscosity, gelation temperature, drug content and in vitro release study. In vivo evaluation for analgesic activity of formulation was carried out in terms of skin irritation study, hot plate method; writhing test and edema paw induce method.</p><p><strong>Results:</strong> The drug content of organogel formulations was found in the range of 92.43±2.10-97.93±0.31% indicating uniform distribution of drug through the base and no interaction of drug with component of base. Posthoc Dunnet’s t-test by employing statistical software, GraphPad InStat 3. It’s shown differences between groups were considered significant at P &lt; 0.05.</p><p><strong>Conclusion:</strong> The transdermal organogel formulation of lornoxicam could provide significant anti-inflammatory and antirheumatic activity when applied topically and was observed to be functional for topical delivery of lornoxicam.</p>


2019 ◽  
Vol 11 (1) ◽  
pp. 43 ◽  
Author(s):  
Madhur Kulkarni ◽  
Vishakha Hastak ◽  
Supriya Jadhav

Objective: The study involved development of transdermal delivery system (TDDS) of doxazosinmesylate (doxa) to achieve effective systemic delivery of the drug.Methods: TDDS of doxa was prepared using hydroxypropyl methyl cellulose (HPMC) K100LV and polyvinyl pyrrolidone (PVP) K30 in 3:1 ratio solvent casting method. The formulation was evaluated for folding endurance, moisture uptake, pH, drug content and in vitro permeation. Various permeation enhancers were incorporated at 5% w/w concentration into the patch formulationto study their impact on the drug permeation. The TDDS made with Transcutol® as an enhancer was subjected to accelerated stability studies and in vivo skin irritation studies.Results: The developed TDDS showed folding endurance of 170, moisture uptakeof 15.7%, pH of 6.3, and drug content of 99±1.1% and 66% in vitro permeation of doxa over 24h. The effect of various enhancers expressed in terms of average flux can be summarized as Transcutol® (10.6±2.1 µg/cm2h)>dimethyl sulfoxide(10.17±1.2 µg/cm2h)>benzyl alcohol (9.55±1.3 µg/cm2h)>no enhancer (8.86±1.1 µg/cm2h)>dimethyl isosorbide (8.21±1.5 µg/cm2h)>Isostearic acid (7.82±1.4 µg/cm2h)>propylene carbonate (7.67±1.4 µg/cm2h)>oleic acid (7.12 µg±0.8/cm2h). The formulation was found to be stable during the accelerated stability studies. In vivo studies indicated absence of skin irritation effect the TDDS containing Transcutol®.Conclusion: TDDS of doxa comprising HPMC K100LV and PVPK30 in the ratio of 3:1 and 5% Transcutol® could serve as a potential TDDS in the treatment of benign prostatic hyperplasia (BPH) and hypertension.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 112 ◽  
Author(s):  
Eloy Pena-Rodríguez ◽  
Mari Carmen Moreno ◽  
Bárbara Blanco-Fernandez ◽  
Jordi González ◽  
Francisco Fernández-Campos

The alteration of retinoids levels in the skin can cause different disorders in the maturation of epithelial skin cells. Topical administration of these lipophilic molecules is a challenge that can be addressed by encapsulation into drug delivery systems. In this study, retinyl palmitate transferosomes formulated in cream were developed and the increases in the penetration of the active ingredients as well as the biodistribution were evaluated in vitro and in vivo. Transfersomes demonstrated a significant increase in the administration of retinyl palmitate to the epidermis by quantification of the active ingredients in the different layers of the skin, as well as by fluorescence microscopy of biopsies of non-dermatomized pig-ear skin. These results suggest that transfersomes may be an efficient vehicle for the delivery of retinoids to inner layers of the skin, such as the epidermis.


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