Abstract
An oral medication of a molecular targeted drug, lapatinib, is taken regularly to maintain the drug concentration within the desired therapeutic levels. To alleviate the need for such cumbersome administration schedules in several drugs, advanced drug delivery systems (DDSs), which can provide time-controlled and sustained drug release, have recently received significant attention. A biodegradable synthetic polymer, such as polycaprolactone (PCL), is usually used as a carrier material for DDSs. In this paper, lapatinib powder-entrapped, PCL microstructures were fabricated with a precise X-ray lithography-based method. In vitro experiments on HER2 positive-human gastric cancer derived NCI-N87 cells were performed to appraise the drug release characteristics of the fabricated DDSs. The in vitro results indicate that after the X-ray lithography process, the lapatinib powder is still working well and show time- and dose- dependent drug release efficiencies. The cell growth inhibition characteristics of one hundred 40-μm sized microstructures were similar to those of a 1 μM lapatinib solution for over 144 h. In conclusion, the developed lapatinib-entrapped PCL microstructures can be used in molecular targeted delivery and sustained release as effective cancer-targeted DDSs.
Highlights
Chemotherapy represents a mainstay in the treatment of metastatic cancer
This paper developed a novel drug delivery systems (DDSs) that consists of PCL outer layers and a lapatinib-powder core for use in targeted and sustained drug delivery
The silicon wafer with the lapatinib-entrapped PCL films and an X-ray mask was placed together onto a jig, and X-ray synchrotron radiation was exposed throughout the jig by controlling the scanning servo motor system
Summary
Chemotherapy represents a mainstay in the treatment of metastatic cancer. its efficacy has been demonstrated against most types of solid tumors, chemotherapy has two critical drawbacks: Toxicity and non-selectivity. We found the anti-tumor activity of lapatinib in gastric cancer with in vitro and in vivo molecular-based approaches, which can be used for targeted drug delivery [23,24,25]. (PLA), and polycaprolactone (PCL), have been used as DDS carriers Among these polymers, PCL is most commonly selected for the following reasons: (1) its slow degradation typically taking two to three years to dissolve, which is suitable for controlled and sustained drug release; (2) its proven stability in serum; (3) its low material costs; and (4) the ability to use common microfabrication methods for DDSs [32,33]. This paper developed a novel DDS that consists of PCL outer layers and a lapatinib-powder core for use in targeted and sustained drug delivery. The drug release characteristics of the fabricated DDS were evaluated with in vitro experiments in NCI-N87 cells
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