Physico-chemical characterisation, cytotoxic activity, and biocompatibility studies of tamoxifen-loaded solid lipid nanoparticles prepared via a temperature-modulated solidification method.
BACKGROUND
Solid lipid nanoparticles (SLNs) can efficiently and efficaciously incorporate anti-cancer agents.


OBJECTIVE
To prepare and characterise tamoxifen (TAM)-loaded SLNs.


METHODS
Glyceryl monostearate, Tween-80, and trehalose were used in SLNs. SLNs were tested via dynamic light scattering (DLS), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FTIR).


RESULTS
Characterisation studies revealed SLNs of about 540 nm with a negative surface charge and confirmed the entrapment of TAM in the SLNs. The entrapment efficiency was estimated to be 60%.


CONCLUSIONS
The in vitro drug release profile demonstrated a gradual increase followed by a release plateau for several days. A drug concentration-dependent increase in cytotoxic activity was observed when the SLNs were evaluated in cell cultures.


CONCLUSIONS
Biocompatible and stable lyophilised SLNs were successfully prepared and found to possess properties that may be utilised in an anti-cancer drug delivery system.
Division of Industrial Pharmacy, Department of Pharmacy Practice, College of Pharmacy and Pharmaceutical Sciences, University of Toledo , Toledo, Ohio , USA .
Sushant
S
Lakkadwala
Sanko
S
Nguyen
Joseph
J
Lawrence
Surya M
SM
Nauli
Jerry
J
Nesamony
D018931:Antineoplastic Agents, Hormonal / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D005989:Glycerides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D008422:Materials Testing; D053758:Nanoparticles / Q000737:chemistry*; D011136:Polysorbates / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D013629:Tamoxifen / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D014199:Trehalose / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
D018931:Antineoplastic Agents, Hormonal; D003692:Delayed-Action Preparations; D005989:Glycerides; D011136:Polysorbates; D013629:Tamoxifen; C048159:glyceryl monostearate; D014199:Trehalose
Biocompatibility; FTIR; X-ray powder diffractometry; dynamic light scattering; solid lipid nanoparticles; zeta potential