In Vitro Anticancer Properties of Linamarin Controlled Release From Biodegradable Poly-Lactic Co-Glycolic Acid Nanoparticle
There are many interests in finding new chemotherapeutic agents for cancer. The current work involved screening of linamarin as the therapeutic agent on different cancer cells, as no such study has been performed previously. Improved bioavailability and delivery of the linamarin to the targeted t...
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| Format: | Thesis |
| Language: | English English |
| Published: |
2005
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| Subjects: | |
| Online Access: | http://psasir.upm.edu.my/id/eprint/5996/1/FK_2005_12.pdf http://psasir.upm.edu.my/id/eprint/5996/ |
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| Summary: | There are many interests in finding new chemotherapeutic agents for cancer. The current
work involved screening of linamarin as the therapeutic agent on different cancer cells, as
no such study has been performed previously. Improved bioavailability and delivery of
the linamarin to the targeted tumour cells can be engineered by proper selection of its
carrier. There are many advantages of choosing biodegradable nanoparticles as a drug
carrier. These include an improved bioavailability and efficacy of the drug. It also offers
a controlled release mechanism in which the activity of the drug can be prolonged at the
affected sites. Besides, the biodegradability character of the carrier means these particles
are easily dissolved in the system without exerting any side effects to the body. The present study investigated fabrication of linamarin encapsulation into biodegradable
nanoparticles to kill cancer cells.
The present study was initiated with an investigation of the toxic effect of linamarin on
cancer cells and their cell cycles. The in vitro study on the effect of linamarin was
performed on two tumour cell lines, HeLa (cervical tumour cell line) and CAOV3
(ovarian tumour cell line). The cytotoxicity of linamarin was determined by the MTT
assay. Both cell lines showed significant cell death when exposed to linamarin with the
IC50 values well within the efficacious limit (IC50 of 30 mglml and 58 mglml for HeLa
and CAOV3 cell lines, respectively, when exposed to pure linamarin). This result
indicated that linamarin has the potential as a for drug candidate for cancer treatment.
The subsequent cell cycle analysis performed by flow cytometry to determine the arrested
point of linamarin within the cell cycle. Results showed significant effect of linamarin on
the G1 phase of the cell cycle. In other words, a significant number of cells were being
arrested in the G1 phase. However, no significant effect was observed on the S and G2-M
stage of the cell cycle stage after treatment with the linamarin for 24 hours.
The second part of the study was on fabrication of biodegradable linamarin loaded
nanoparticles. Poly (lactic-co-glycolic acid) (PLGA) was chosen as the polymeric
material of the nanoparticles. The water-in-oil-in-water emulsification process was the
method of choice for the encapsulation of linamarin inside polymeric particles. The
linamarin nanoparticles based on two different mole fraction of PLGA copolymer (50150
and 85150 of lactic acidglycolic acid, respectively) were successfully fabricated using
water-in- oil-in-water double emulsion extractionlevaporation technique. The SEM analysis on the morphologies of the nanoparticles showed the particles are spherical in
shape with porous surface structure and well within nano-scale in size.
A preliminary investigation on in vitro drug (linamarin) release was also carried out. The
in vitro drug (linamarin) release was characterised by an initial burst and incomplete
dissolution of the drug. When decreasing the polymer/drug ratio, the release appeared
more controlled and prolonged up to 8hr. It can be concluded that nanoparticles prepared
by water-in-oil-in-water emulsification followed by solvent evaporation is a good
potential for a controlled released-drug carriers for linamarin. |
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