Development and evaluation of hyaluronic acid conjugated tacrolimus-loaded nanostructured lipid carriers using moringa oleifera seed oil as liquid lipid

The proposed research work aims to develop hyaluronic acid conjugated tacrolimus-loaded nanostructured lipid carriers (HYA-TAC-loaded-SA-NLCs) to improve the release rate and cellular uptake to enhance its oral absorption. TAC-loaded-SA-NLCs were prepared using stearylamine as solid lipid and Moringa oleifera (MO) seed oil. The conjugation of hyaluronic acid (HYA) to the surface of TAC-loaded-SA-NLCs was done using electrostatic interaction between stearylamine and HYA. Further, the conjugation is confirmed by using zeta potential and FTIR (Fourier transform infrared) spectroscopy.

In-vitro release study showed ∼12 and ∼11 times more drug dissolution efficiency from TAC-loaded-SA-NLCs and HYA-TAC-loaded-SA-NLCs than TAC-suspension. The in-vitro protein denaturation studies showed that HYA-TAC-loaded-SA-NLCs had a lower IC₅₀ than TAC-loaded-SA-NLCs and TAC suspension. Furthermore, the cellular uptake studies in HCT-116 cells showed enhanced cellular uptake of unmodified NLCs (∼2.5 times) and HYA modified NLCs (∼8.4 times) than suspension. The storage stability study revealed no significant change in the lyophilized HYA-TAC-loaded-SA-NLCs after 3 months. Hence, the study concluded that the prepared HYA modified NLCs could significantly improve the cellular uptake and anti-inflammatory activity.

Materials

Tacrolimus (TAC), Moringa oleifera seed oil (MO) and egg albumin were purchased from Yarrow Chem Products Pvt. Ltd. Mumbai, Hyaluronic acid (HYA) was purchased from chemdyes corporation, d-α-Tocopherol polyethylene glycol succinate (TPGS) was purchased from Sigma-Aldrich, stearylamine was purchased from Central Drug House Pvt. Ltd. Delhi, Poloxamer 188 was purchased from HiMedia Laboratories Pvt. Ltd. Mumbai, Water (HPLC grade) was purchased from Thermo Fisher Scientific India Pvt. Ltd

Rajat Garg, Anuj Garg, Development and evaluation of hyaluronic acid conjugated tacrolimus-loaded nanostructured lipid carriers using moringa oleifera seed oil as liquid lipid, Journal of Drug Delivery Science and Technology, Volume 95, 2024, 105591, ISSN 1773-2247, https://doi.org/10.1016/j.jddst.2024.105591.