Nano-Fibular Nanoparticle Polymer-Drug Conjugate for Sustained Dermal Delivery of Retinoids
This technology has applications in the treatment of acne and skin diseases, as well as the development of anti-aging products.
Researchers
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nano-fibular nanoparticle polymer-drug conjugate for sustained dermal delivery of retinoids
United States of America | Granted | 11,590,240
Figures
Schematic of the nanomicelle fibular structures, composed of ATRA particles bound to poly- (vinyl alcohol) via DCC chemistry, showing penetration into the dermis. The ATRA is released in the hydrated dermis.
Technology
In comparison to previously existing approaches, this technology conjugates ATRA to an FDA approved, soluble polymer through an ester-bond linkage, creating water-soluble polymer-drug nanomicelles with controlled ATRA release characteristics. The ATRA is conjugated to poly-(vinyl alcohol) (PVA) by DCC chemistry in a one-pot synthesis reaction. These nanomicelles have high aspect ratio nanofiber structures which facilitate uptake into the dermis while at the same time reducing mobility in the tissue, thereby enforcing controllable ATRA release. In vitro studies demonstrate ATRA as an effective anti-proliferative. In vivo studies in mice suggest that these nanomicelles ensure controlled release of ATRA, reducing irritation and inflammation at the sight of interest and promoting application and retention of the structures. The new technology could find applications in treatment of acne and skin diseases, improving therapy efficacy and reducing side effects with more controlled delivery mechanisms, while allowing for a user friendly, non-greasy formulation of the active agent.
Problem Addressed
Retinoids are a broadly used class of therapeutics. All-trans retinoic acid (ATRA), in particular, has been widely used in formulations for anti-aging and wrinkle reduction, in addition to being a first line cancer therapy in lymphoblastic leukemia. The challenge in ATRA delivery is that the molecules are very hydrophobic, making them water-insoluble, so formulations of ATRA rely on emulsifiers that are greasy and may damage areas of application. This technology introduces a novel, non-greasy formulation to deliver all-trans retinoic acid (ATRA) for cosmetic applications.
Advantages
- Includes a non-greasy formulation due to water solubility of nanomicelles
- Better control of ATRA delivery and reduction of side-effects such as irritation and inflammation
- PATRA (PVC-bound ATRA) synthesis is easily scalable
- Improved stability of ATRA as the ATRA-bound polymer protects it from light degradation
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