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Published on: November 1, 2017
Quality by Design-Endorsed Nilotinib-Laden Liposomal Gel for Enhanced Dermal Delivery in Melanoma Management:
Aachal Hedaoo1, Pooja Khairnar1, Ganesh Vambhurkar1
1Pharmaceutical Innovation and Translational Research Lab (PITRL), Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana 500037, India.
Abstract:
Melanoma, a malignant form of skin cancer, is associated with high mortality owing to its high metastasis rate. Migration and invasion of the malignant tumor cells are the prime reasons behind the poor 5-year survival rate of patients after diagnosis. The primary objective of this study was to fabricate a topically effective liposome-based platform for the deeper penetration of nilotinib (NTB) for effective melanoma management. In this study, nilotinib-loaded liposomes (NTB-loaded LPS) were fabricated and further embedded within a Sepineo P600-based gel. Particle size, PDI, and zeta potential of the NTB-loaded LPS were found to be 135 ± 2.94 nm, 0.136 ± 0.02, and -27.7 ± 0.12 mV, respectively. TEM analysis revealed that the NTB-loaded LPS exhibits uniform spherical particles with a size of ∼140 nm. Drug loading and entrapment efficiency of NTB-loaded LPS were 4.61 ± 0.24% and 79.66 ± 2.62%, respectively. The cytotoxicity study revealed that the IC50 values of NTB and NTB-loaded were found to be 12.5 ± 1.35 μM and 6.25 ± 2.48 μM, respectively. Quantitative and qualitative cellular uptake studies demonstrated that NTB-loaded LPS were successfully internalized within B16-F10 cells. Results from the Annexin V apoptosis assay revealed that the NTB-loaded LPS enhanced the early (7.27-fold) and late-stage apoptosis (3.2-fold) compared to the free NTB and thereby contributes to the overall cytotoxic potential of NTB. Therefore, the in vitro cellular studies depict that the NTB-loaded LPS successfully inhibit the proliferation, migration, and invasion of the melanoma cells. The ex vivo skin permeation study signifies that the NTB-loaded LPS gel improved the permeation and retention of NTB by 3.1- and 2.6-fold, respectively, compared to the plain NTB-loaded gel. Collectively, these findings highlight the potential of NTB-loaded liposomal gel as an effective, noninvasive, and patient-friendly approach for melanoma management.
