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Chitooligosaccharides Modified Reduction-Sensitive Liposomes: Enhanced Cytoplasmic Drug Delivery and
Xuelei Yin1, Yingying Chi1, Chuanyou Guo2
1School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai, 264005, People's Republic of China.
Chitosan oligosaccharide (COS) coated liposomes are reduction-sensitive, enhancing tumor cell drug delivery and efficacy. These novel liposomes improve drug loading, cellular uptake, and antitumor effects in animal models.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Drug Delivery Systems
Background:
- Liposomes are widely used for drug delivery, but achieving targeted cytoplasmic delivery remains a challenge.
- Developing stimuli-responsive systems that release drugs within target cells can improve therapeutic efficacy and reduce side effects.
Purpose of the Study:
- To create reduction-sensitive and fusogenic liposomes coated with chitosan oligosaccharides (COS) via a disulfide linker for targeted cytoplasmic drug delivery.
- To evaluate the potential of these liposomes for enhanced anticancer drug delivery and efficacy.
Main Methods:
- Chitosan oligosaccharides (COS) were chemically tethered to cholesterol (Chol) via a disulfide linker (-SS-) on liposomes.
- Doxorubicin (DOX) was loaded into the liposomes, and their reduction-sensitivity, cellular uptake, cytotoxicity, pharmacokinetics, and antitumor efficacy were assessed.
- Liposomes were characterized for size, zeta potential, and drug loading capacity.
Main Results:
- Chol-SS-COS/DOX liposomes (100 nm) showed high drug loading (13% w/w) and stability under physiological conditions, but destabilized in the presence of reducing agents (DTT or GSH) at cytosolic concentrations.
- These liposomes exhibited enhanced cytotoxicity to MG63-osteosarcoma cells compared to non-reduction sensitive counterparts.
- Flow cytometry and confocal microscopy confirmed efficient cellular internalization and cytoplasmic drug delivery of Chol-SS-COS/DOX, with preferential uptake by cancer cells over normal liver cells.
- In vivo studies demonstrated a prolonged half-life of DOX and significant inhibition of tumor growth in mice, along with extended survival rates.
Conclusions:
- Reduction-responsive Chol-SS-COS liposomes represent a promising platform for effective cytoplasmic delivery of anticancer drugs.
- Conjugation of liposomes with COS significantly enhances tumor cell uptake, antitumor activity, and survival rates in preclinical models.
