Exploring the potential of oleic acid in nanotechnology-mediated dermal drug delivery: An up-to-date review

Author(s):  
Bassant Atef ◽  
Rania A.H. Ishak ◽  
Sabry S. Badawy ◽  
Rihab Osman
Nanomaterials ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 2323
Author(s):  
Olga Pelikh ◽  
Cornelia M. Keck

Many active pharmaceutical ingredients (API) possess poor aqueous solubility and thus lead to poor bioavailability upon oral administration and topical application. Nanocrystals have a well-established, universal formulation approach to overcome poor solubility. Various nanocrystal-based products have entered the market for oral application. However, their use in dermal formulations is relatively novel. Previous studies confirmed that nanocrystals are a superior formulation principle to improve the dermal penetration of poorly soluble API. Other studies showed that nanocrystals can also be used to target the hair follicles where they create a drug depot, enabling long acting drug therapy with only one application. Very recent studies show that also the vehicle in which the nanocrystals are incorporated can have a tremendous influence on the pathway of the API and the nanocrystals. In order to elucidate the influence of the excipient in more detail, a systematic study was conducted to investigate the influence of excipients on the penetration efficacy of the formulated API and the pathway of nanocrystals upon dermal application. Results showed that already small quantities of excipients can strongly affect the passive dermal penetration of curcumin and the hair follicle targeting of curcumin nanocrystals. The addition of 2% ethanol promoted hair follicle targeting of nanocrystals and hampered passive diffusion into the stratum corneum of the API, whereas the addition of glycerol hampered hair follicle targeting and promoted passive diffusion. Propylene glycol was found to promote both pathways. In fact, the study proved that formulating nanocrystals to improve the bioefficacy of poorly soluble API upon dermal application is highly effective. However, this is only true, if the correct excipient is selected for the formulation of the vehicle. The study also showed that excipients can be used to allow for a targeted dermal drug delivery, which enables to control if API should be delivered via passive diffusion and/or as drug reservoir by depositing API in the hair follicles.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 804
Author(s):  
Ágnes Bajza ◽  
Dorottya Kocsis ◽  
Orsolya Berezvai ◽  
András József Laki ◽  
Bence Lukács ◽  
...  

The efficacy of transdermal absorption of drugs and the irritation or corrosion potential of topically applied formulations are important areas of investigation in pharmaceutical, military and cosmetic research. The aim of the present experiments is to test the role of P-glycoprotein in dermal drug delivery in various ex vivo and in vitro platforms, including a novel microchip technology developed by Pázmány Péter Catholic University. A further question is whether the freezing of excised skin and age have any influence on P-glycoprotein-mediated dermal drug absorption. Two P-glycoprotein substrate model drugs (quinidine and erythromycin) were investigated via topical administration in diffusion cells, a skin-on-a-chip device and transdermal microdialysis in rat skin. The transdermal absorption of both model drugs was reduced by P-glycoprotein inhibition, and both aging and freezing increased the permeability of the tissues. Based on our findings, it is concluded that the process of freezing leads to reduced function of efflux transporters, and increases the porosity of skin. P-glycoprotein has an absorptive orientation in the skin, and topical inhibitors can modify its action. The defensive role of the skin seems to be diminished in aged individuals, partly due to reduced thickness of the dermis. The novel microfluidic microchip seems to be an appropriate tool to investigate dermal drug delivery.


2021 ◽  
pp. 693-714
Author(s):  
Gøril Eide Flaten ◽  
Nataša Škalko-Basnet ◽  
Željka Vanić

2011 ◽  
Vol 23 (01) ◽  
pp. 29-35
Author(s):  
Chin-Hsiung Hsieh ◽  
Yuan-An Ku ◽  
Lien-Hua Chiu ◽  
Tai-Horng Young ◽  
Yi-You Huang

Patients with beta-thalassaemia major need blood transfusion frequently during their whole life. However, frequent transfusions will eventually lead to the accumulation of trivalent iron, resulting in iron overload. To reduce iron overload, patients are administered regularly with intravenous or subcutaneous infusion of deferioxamine mesylate (DFO). Nevertheless, high costs of medication, poor patient compliance, and side effects limit its use and patient's acceptance. To overcome such drawbacks, we developed a novel transdermal delivery system to administer the DFO instead of traditional injections. We assayed the feasibility of fabricating a transdermal DFO patch using the single-layer drug-in-adhesive drug delivery system. We used the pressure-sensitive adhesives and hydrogels as the drug reservoirs and studied the release profile of DFO from the transdermal patches in vitro. In order to enhance the transdermal delivery rate, chemical enhancers, polysorbate 80 and oleic acid, and physical enhancer, ultrasound, were incorporated into the monolith DFO patches. Experimental results showed that the combination of polysorbate 80 and oleic acid in the pressure-sensitive adhesives enhanced the penetration efficiency through nude mice skin. The pretreatment of nude mice skin with ultrasound temporally changed the diffusional resistance and facilitated DFO penetration through the skin. We expect that the new delivery system can enable the drug to penetrate through skin at a stable rate and reach the circulation system successfully, thus allowing the concentration of drug to achieve the therapeutic effect.


2017 ◽  
Vol 8 (12) ◽  
pp. 1077-1096 ◽  
Author(s):  
Kaushalkumar Dave ◽  
Venkata Vamsi Krishna Venuganti

Proceedings ◽  
2017 ◽  
Vol 1 (4) ◽  
pp. 304 ◽  
Author(s):  
Yuki Nabekura ◽  
Hitoshi Fukuyu ◽  
Yoshihiro Hasegawa ◽  
Mitsuhiro Shikida

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