AAPS PharmSciTech

, Volume 19, Issue 3, pp 1344–1357 | Cite as

Facile Synthesis of Chitosan Capped Mesoporous Silica Nanoparticles: A pH Responsive Smart Delivery Platform for Raloxifene Hydrochloride

  • Priya V. Shah
  • Sadhana J. Rajput
Research Article


An encapsulation of model drug raloxifene hydrochloride (RAL) inside the chitosan decorated pH responsive mesoporous system has a greater potential for accumulating in the tumor cells. The present study involves synthesis of surface modified mesoporous silica nanoparticles (MSN) with the aim of achieving pH sensitive drug delivery system. A silanol skeleton of MSN has been productively modified to amine intermediate which served as a firm platform to adapt chitosan grafted assembly and systematically evaluated. RAL incorporation inside the featured mesopores was performed employing novel immersion solvent evaporation methodology and evaluated further. The pH responsive behavior of formulated nano framework was studied at three different pH of a phosphate buffer saline individually. The in vitro cell viability assay on MCF-7 breast carcinoma cells was performed in time and concentration dependent manner. Finally, the hemolysis assay of designed nanoparticle was accomplished to envisage the hemocompatibility. The outcome of characterization details unveiled a perfect 2D hexagonal spherical structure gifted with higher surface area and optimum pore size for designed nanoparticles. The higher percentage grafting of amine and chitosan residue, i.e., 4.01 and 28.51% respectively along with 31.89 and 33.57% RAL loading efficiency made MSNs more attractive and applicable. Eventually, in vitro release study exhibited higher RAL release in acidic media for extended time periods confirming successful formation of pH responsive nanoparticle having controlled release property. Conclusively potential of designed nanosystem to serve efficient anti-cancer remedy was confirmed by superior behaviour of chitosan grafted MSN towards MCF-7 cells with supreme hemocompatibility.


raloxifene hydrochloride anomalous release chitosan MCF-7 hemolysis assay 



The authors thank Dr. Amirali Popat, School of Pharmacy, The University of Queensland, Australia and Zydus research centre, Gujarat, India for providing RAL gift sample.

Compliance with Ethical Standards

Conflict of Interest

The authors declare that they have no conflict of interest.

Supplementary material

12249_2017_949_MOESM1_ESM.jpg (78 kb)
Supplementary figure 1 FT-IR spectra of (A) RAL; (B) RAL@CTAB; (C) MSN-41 (D) MSN-NH2–41 (E) MSN-CHITO-41 (F) RAL-41 (G) RAL-NH2–41 (H) RAL-CHITO-41 (JPEG 77 kb)
12249_2017_949_MOESM2_ESM.jpg (28 kb)
Supplementary figure 2 DSC thermogram of (A) RAL; (B) RAL-41; (C) RAL-NH2–41 (D) RAL-CHITO-41 (JPEG 28 kb)
12249_2017_949_MOESM3_ESM.jpg (86 kb)
Supplementary figure 3 Hydrodynamic pore size distribution pattern for (A) MSN-41; (B) MSN-NH2–41 (C) MSN-CHITO-41 (JPEG 86 kb)
12249_2017_949_MOESM4_ESM.jpg (45 kb)
Supplementary figure 4 Supplementary fig. 4: (A) DSC and (B) WAXS data for RAL after solvent evaporation (JPEG 44 kb)
12249_2017_949_MOESM5_ESM.jpg (37 kb)
Supplementary figure 5 TGA thermogram of (A) RAL; (B) RAL-41; (C) RAL-NH2–41 (D) RAL-CHITO-41 (JPEG 36 kb)
12249_2017_949_MOESM6_ESM.jpg (24 kb)
Supplementary figure 6 TGA thermogram of (A) MSN-41; (B) MSN-NH2–41 (C) MSN-CHITO-41 (JPEG 23 kb)


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Copyright information

© American Association of Pharmaceutical Scientists 2018

Authors and Affiliations

  1. 1.Faculty of Pharmacy, Centre of Relevance and Excellence in New Drug Delivery System, Government of IndiaThe Maharaja Sayajirao University of BarodaVadodaraIndia

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