Nanostructured Lipid Carriers (NLC) for Parenteral Delivery of an Anticancer Drug |
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Authors: | Akhayacatra Chinsriwongkul Ponwanit Chareanputtakhun Tanasait Ngawhirunpat Theerasak Rojanarata Warisada Sila-on Uracha Ruktanonchai Praneet Opanasopit |
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Institution: | (1) Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand;(2) Faculty of Pharmacy, Ubon-Rajathanee University, Ubon-Rajathanee, Thailand;(3) National Nanotechnology Center (Nanotec), Pathum Thani, Thailand; |
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Abstract: | The purpose of this research was to formulate nanostructured lipid carriers (NLC) for the parenteral delivery of an anticancer
drug, all-trans retinoic acid (ATRA). The ATRA was incorporated into NLC by the de novo emulsification method. The effect of the formulation
factor, i.e., type and oil ratio, initial ATRA concentration on physicochemical properties was determined. The anticancer
efficacy of ATRA-loaded NLC on HL-60 and HepG2 cells was also studied. NLC was formulated using a blend of solid lipids (cetyl
palmitate) and liquid lipids (soybean oil (S), medium-chain triglyceride (M), S/oleic acid (O; 3:1) and M/O (3:1)) at a weight
ratio of 1:1. ATRA-loaded NLC had an average size of less than 200 nm (141.80 to 172.95 nm) with a narrow PDI and negative
zeta potential that was within an acceptable range for intravenous injection. The results indicated that oleic acid enhanced
the ATRA-loading capacity of NLC. In vitro ATRA release was only approximately 4.06% to 4.34% for 48 h, and no significant difference in ATRA release rate from all
NLC formulations in accordance with the composition of the oil phase. Moreover, no burst release of the drug was observed,
indicating that NLC could prolong the release of ATRA. The initial drug concentration affected the photodegradation rate but
did not affect the release rate. All ATRA-loaded NLC formulations exhibited the photoprotective property. The cytotoxicity
results showed that all ATRA-loaded NLC had higher cytotoxicity than the free drug and HL-60 cells were more sensitive to
ATRA than HepG2 cells. |
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