Lactoferrin-tagged quantum dots-based theranostic nanocapsules for combined COX-2 inhibitor/herbal therapy of breast cancer.

AIM: Herein, tumor-targeted quantum dots (QDs)-based theranostic nanocapsules (NCs) coloaded with celecoxib and honokiol were developed. Materials & methodology: The anionic CD44-targeting chondroitin sulfate and cationic low density lipoprotein (LDL)-targeting lactoferrin (LF) were sequentially assembled onto the surface of the positively charged oily core. As an imaging probe, highly fluorescent mercaptopropionic acid-capped cadmium telluride QDs were coupled to LF. RESULTS: In vitro, fluorescence of QDs was quenched (OFF state) due to combined electron/energy transfer-mediated processes involving LF. After intracellular uptake of NCs, fluorescence was restored (ON state), thus enabled tracing their internalization. The NCs demonstrated enhanced cytotoxicity against breast cancer cells as well as superior in vivo antitumor efficacy. CONCLUSION: We propose these multifunctional nanotheranostics for imaging and targeted therapy of breast cancer.

Layer-by-layer gelatin/chondroitin quantum dots-based nanotheranostics: combined rapamycin/celecoxib delivery and cancer imaging.

Aim: Nanotheranostics consisting of highly-fluorescent quantum dots coupled with gelatin/chondroitin layer-by-layer assembled nanocapsules were developed. Materials & methods: The hydrophobic drugs celecoxib (CXB) and rapamycin (RAP) were co-loaded into the oily core of nanocapsules (NCs) to enable synergistic growth inhibition of breast cancer cells. To overcome the nonspecific binding of actively targeted CS-NCs with normal cells, a matrix metalloproteinase (MMP-2)-degradable cationic gelatin layer was electrostatically deposited onto the surface of the negatively-charged CS-NCs. Results: The prepared nanocarriers displayed strong fluorescence which enabled tracing their internalization into cancer cells. An enhanced cytotoxicity of the NCs against breast cancer cells was demonstrated. In vivo, the nanoplatforms displayed superior antitumor efficacy as well as nonimmunogenic response. Conclusion: Therefore, these multifunctional nanoplatforms could be used as potential cancer theranostics.

Development and optimization of a novel drug free nanolipid vesicular system for treatment of osteoarthritis.

OBJECTIVE: The goal of this study is to improve the transdermal delivery of phosphatidylcholine (PC) via constructing a novel nanolipid vesicular system (NLVS) with high level of permeability through the stratum corneum (SC). SIGNIFICANCE: In our study, a novel drug free NLVS was developed. The system depends on PC boundary cartilage lubrication to relieve osteoarthritic pain without developing gastrointestinal problems associated with anti-inflammatory drug. MATERIALS AND METHODS: A full two-level (23) factorial design is applied to optimize the quality of the prepared NLVS. The selected independent variables are the concentration of PC, the concentration of edge activator (EA), and EA type. The developed NLVS was evaluated for in-vitro, ex-vivo as well as in-vivo efficacy in rat animal model. RESULTS: Based on the factorial design, the selected formulation variables significantly affect the tested responses. The prepared NLV formulations have a particle size (PS)in the range of 10.34 to 496.3 nm, polydispersity index (PdI) values less than one, and negative zeta potential (ZP) range of -1.42 to -32.01 mV. In-vitro and ex-vivo study results reveal that the designed NLVS is effective in sustaining PC release and enhancing its transdermal permeation over 24 h. The optimal permeation flux through ex-vivo study is 0.415 mg/cm2/h following zero-order kinetics. Moreover, in-vivo study of the optimized formulations demonstrated remarkable reduction in inflammatory mediators associated with osteoarthritis (OA). CONCLUSION: The results indicate that the optimized drug free NLVS significantly augment transdermal delivery of PC and have a potential role in treatment of OA without the risk of systemic side effects.