Polylactic Acid and Polycaprolactone Blended Cosmetic Microneedle for Transdermal Hispidin Delivery System

Abstract

Microneedles (MNs) are a new system of effective drug delivery that create micron-sized pathways to the epidermis or upper dermis regions of the skin. In this study, we developed coated-type microneedles for direct hispidin delivery to the skin. Hispidin is a well-known plant-derived antioxidant component showing antitumor, anti-inflammatory, antiallergic, antiangiogenic, antioxidant, hypoglycemic, hypolipidemic, and immunomodulatory activities. Polymeric blends of polylactic acid (PLA) and polycaprolactone (PCL) were casted as MNs to enhance skin permeability. PLA/PCL MNs exhibited the highest strength of 51.26 MPa with a width of ~200 ųm. Hispidin was directly coated onto the MNs with PLA/PCL blends to form delivery layers. Compared to the hispidin-only delivery layer, skin permeability of hispidin increased by over 50% when using agarose gel in in vitro tests. In a dose-dependent manner, hispidin coated on PLA/PCL MNs also showed a brightening effect, as well as anti-inflammatory activity at the gene and protein level in skin cell culture experiments. It also demonstrated antimicrobial activity, and showed no cytotoxicity to skin cells. These results suggest that the PLA/PCL MN system with hispidin may have great potential as a prototype platform for various drug delivery systems, allowing the development of more effective subcutaneous delivery of vaccines, oligonucleotides, insulin, and many other cosmetic applications.

A Novel Approach for Glycero-(9,10-trioxolane)-Trialeate Incorporation into Poly(lactic acid)/Poly(ɛ-caprolactone) Blends for Biomedicine and Packaging

“…Sorption characteristics at room temperature do not appear for this film. The study was carried out at a temperature of 35 °C, since the intended possible applications of developed mixed PLA/PCL films assume their use in direct contact with human skin [ 57 , 58 ]. The structure of the OTOA molecule consists mainly of hydrophobic fragments and includes, along with low-polar ester groups, specific ozonide rings [ 59 ].…”

A Novel Approach for Glycero-(9,10-Trioxolane)-Trialeate Incorporation into Poly(lactic Acid)/Poly(ɛ-Caprolacton) Blends for Biomedicine and Packaging

“…The study was carried out at a temperature of 35 °C, since the intended possible applications of developed mixed PLA/PCL films assume their use in direct contact with human skin [57,58]. The structure of the OTOA molecule consists mainly of hydrophobic fragments and includes, along with low-polar ester groups, specific ozonide rings [59]. Only for PLA/PCL film with 40% OTOA observed sorption characteristics were similar to those of PCL films.…”

Controlled degradation of polycaprolactone-based micropillar arrays

“…38 Recently, similar work by Lee et al demonstrated that PCL/PLA blends of varying concentrations could achieve microneedles with great mechanical strengths (up to 51.26 MPa) for the transdermal delivery of hispidin. 39 Understanding the degradation, solubility and biocompatibility of such structured materials is essential for wide ranging applications in controlled drug release and delivery and implantable medical devices. The presence of specific degradable functionalities within the polymer chain is crucial for degradation to occur and by varying the concentration of such functional groups, control over degradability and the rate of degradation can be achieved.…”

“… 38 Recently, similar work by Lee et al demonstrated that PCL/PLA blends of varying concentrations could achieve microneedles with great mechanical strengths (up to 51.26 MPa) for the transdermal delivery of hispidin. 39 …”