Chitosan microparticles as entrapment system for trans- cinnamaldehyde: Synthesis, drug loading, and in vitro cytotoxicity evaluation

The ionic gelation method was used to study the effect of the crosslinking agent, sodium tripolyphosphate on average particle size (Dp) and zeta potential (ζp) of chitosan microparticles (CSMP) unloaded and loaded with trans-cinnamaldehyde (TCIN). The obtained values of Dp and ζp trend as 117.6 ± 0....

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Bibliographic Details
Published in:International journal of biological macromolecules 2021-01, Vol.166, p.322-332
Main Authors: Barrera-Martínez, Cynthia Lizeth, Padilla-Vaca, Felipe, Liakos, Ioannis, Meléndez-Ortiz, Héctor Iván, Cortez-Mazatan, Gladis Y., Peralta-Rodríguez, René Darío
Format: Article
Language:English
Subjects:
Acrolein - administration & dosage
Acrolein - analogs & derivatives
Acrolein - toxicity
Animals
Antineoplastic Agents, Phytogenic - administration & dosage
Antineoplastic Agents, Phytogenic - toxicity
Cell Proliferation - drug effects
Chitosan
Chitosan - chemistry
Cross-Linking Reagents - chemistry
Dogs
Drug Liberation
HeLa Cells
Humans
Hydrogels - chemistry
Madin Darby Canine Kidney Cells
MDCK cells
Microparticles
Microspheres
Trans-cinnamaldehyde
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Summary:The ionic gelation method was used to study the effect of the crosslinking agent, sodium tripolyphosphate on average particle size (Dp) and zeta potential (ζp) of chitosan microparticles (CSMP) unloaded and loaded with trans-cinnamaldehyde (TCIN). The obtained values of Dp and ζp trend as 117.6 ± 0.4 ≤ Dp ≤ 478.5 ± 3.5 nm and +27.8 ± 1.3 ≤ ζp ≤ +103.5 ± 4.2 mV, respectively. The entrapment efficiency of TCIN in CSMP was 9.1 ± 2.0% and 71.5 ± 2.9% was released after 360 min (pH = 6.5) which reveals a potential anti-cancer activity in acidic environment. Cytotoxicity of TCIN in DMSO (0–50 μM) was evaluated on MDCK and HeLa cell lines and exhibited low effect at either 24 or 48 h of exposure; whereas TCIN-loaded CSMP (0–50 μM) showed, after 24 h of exposure, 67.6 ± 7.0 and 64.5 ± 3.9% cytotoxicity for MDCK and HeLa cell lines, respectively. At 48 h of exposure, TCIN-loaded CSMP achieved 81.1 ± 0.26 and 77.9 ± 4.2% cytotoxicity for MDCK and HeLa cell lines, respectively. •TCIN-loaded CSMP significantly enhanced its activity on HeLa cancer cells.•Higher cumulative TCIN releasing was found at pH 6.5 than 7.4 pH.•CSMP shows cytotoxic effects of TCIN on HeLa and MDCK cell lines.•Dp and ζp of the obtained TCIN-loaded CSMP (
ISSN:0141-8130
1879-0003
DOI:10.1016/j.ijbiomac.2020.10.188