Synthesis, Characterisation And Evaluation Of Biocompatible Disulphide Cross-Linked Sodium Alginate Derivative Nanoparticles For Colon Targeted Drug Delivery

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Date
2018-03
Authors
Ayub, Asila Dinie
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Publisher
Universiti Sains Malaysia
Abstract
Colon specific nano-drug delivery is a challenging system for a drug to reach the colon target site without any release along the stomach and small intestines. The application of layer-by-layer (LbL) on nanoparticles surface coating has been applied to improve the colon targeted oral drug delivery of insoluble drugs. Here, we aimed to formulate a self-assembly cysteamine-based disulphide cross-linked sodium alginate (SA) (with LbL) to improve the delivery of paclitaxel to colonic cancer cells to promote oral chemotherapy. Cysteamine was conjugated to the backbone of oxidised SA to form a core of self-assembly disulphide cross-linked nanospheres. Five formulations were formed, P1DL-P5DL and verified by Raman analysis. P3DL was chosen for paclitaxel loading and fabricated (LbL) with poly(allylamine hydrochloride) (PAH) and poly (4-styrenesulfonic acid-co-maleic acid) sodium salt (PSSCMA) after showing promising results from the characterisation and drug release studies. P3DL fabricated paclitaxel loaded nanospheres, P3DL/PAH/PSSCMA exhibited an encapsulation efficiency of 77.1 % with cumulative drug release of 45.1 %. Dynamic Light Scattering (DLS) analysis was reported at 173.6 ± 2.5 nm with polydispersity index of 0.394 ± 0.105 and zeta potential of -58.5 mV. TEM and SEM analyses exhibited spherical shapes of nanoparticles. P3DL/PAH/PSSCMA was pH- dependent swelling transition from the pH sensitivity study (pH 1 to 7, increase of 102.2 %). Meanwhile, the size of the nanospheres increased 33.0 % in reduction-responsive study after incubating in 10 mM glutathione (day 7). The HT-29 cells showed high viabilities (86.7 %) after been treated with the nanospheres at 50 μg/mL.and therefore, it was regarded as promising nanocarrier in colon drug delivery.
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Keywords
Colon specific nano-drug delivery , drug to reach the colon target site
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