Development of transdermal vitamin D3 (VD3) delivery system using combinations of PLGA nanoparticles and microneedles

Abstract

Although vitamin D3 (VD3), which is the main form of vitamin D, can be produced in human skin under the sunlight, vitamin D deficiency emerged as a major public health problem worldwide. Mainly, oral supplements or vitamin D-fortified foods are distributed to help supplementation of vitamin D. However, those oral methods are limitedly supplied in the Middle East countries, and oral absorption has low efficiency due to many barriers and various changes of conditions along the route. Then, it is recommended to take them every day in order to maintain the adequate serum level of vitamin D. Alternatively, transdermal delivery system could provide a convenient way to get sustained supplement of vitamin D by its advantages like avoiding first-pass effect of the liver and providing release for long periods of time. In this study, we introduced transdermal delivery system for sustained vitamin D release using coating microneedles that easily pierce the skin layer with enough mechanical strength and allow the localization of drugs within the dermal region. According to the experimental results, poly (lactic-co-glycolic acid) (PLGA) successfully encapsulated VD3 as a nanoparticle form with appropriate properties for transdermal delivery such as size distribution, skin compatibility, and effective release of encapsulated compound. Finally, PVD3 layers coated on solid microneedles were completely dissolved into intradermal region in porcine skin model and revealed better performance for VD3 release into plasma compared to ointment base transdermal method.

Microneedle-Based Delivery: An Overview of Current Applications and Trends

“…These MNA showed a five-fold better delivery performance than a transdermal cream containing chemical permeation enhancers. In particular, the delivery efficiency was 81.08% of the initial dose for the MNA and only 16.28% for the transdermal cream [142].…”

Microneedle-based drug delivery: materials of construction

“…The particles can be delivered through the conduits of hollow MNs, coated onto solid MNs or encapsulated within dissolving MNs. [129][130][131][132] Figure 5c shows MNs completely prepared form PLA microparticles. Delivery of other therapeutics, especially proteins and vaccines can be enhanced by surface modifications of MNs.…”

Drug Delivery Systems for Vitamin D Supplementation and Therapy

“…It should be explained that microneedles easily pierce the skin layer with enough mechanical strength and allow the localization of drugs within the dermal region. Finally, layers of nanoparticles coated on solid microneedles were dissolved entirely into the intradermal region in the porcine skin model and revealed better performance for VD3 release into the receptor compartment compared to the ointment-based transdermal method [57].…”

“…That is why a significant challenge is to increase the limited drug penetration and to minimize systemic exposure [60,61]. Another issue that should be taken into consideration when developing topical delivery systems is the high sensitivity of VD3 to external environmental factors such as light, heat, and oxygen [57]. The success of drug delivery depends, among other things, on the physicochemical properties of the active and its carriers in the formulation.…”