RT Unpublished Material
T1 Pegylated lipid nanocapsules with improved drug encapsulation and controlled release properties
A1 Hervella, Pablo
A1 Alonso-Sande, Maria
A1 Ledo, Francisco
A1 Lucero, Maria L.
A1 Alonso Fernández, María José
A1 García-Fuentes, Marcos
K1 Nanomedicine
K1 Nanocapsules
K1 Targeting
K1 Cancer therapy
K1 Encapsulation
K1 Controlled release
AB Drugs with poor lipid and water solubility are some of the most challenging to formulate in nanocarriers, typically resulting in low encapsulation efficiencies and uncontrolled release profiles. PEGylated nano- capsules (PEG-NC) are known for their amenability to diverse modifications that allow the formation of domains with different physicochemical properties, an interesting feature to address a drug encapsulation problem. We explored this problem by encapsulating in PEG-NC the promising anticancer drug candidate F10320GD1, used herein as a model for compounds with such characteristics. The nanocarriers were pre- pared from Miglyol®, lecithin and PEG-sterate through a solvent displacement technique. The resulting system was a homogeneous suspension of particles with size around 200 nm. F10320GD1 encapsulation was found to be very poor (<15%) if PEG-NC were prepared using water as continuous phase; but we were able to improve this value to 85% by fixing the pH of the continuous phase to 9. Interestingly, this modification also improved the controlled release properties and the chemical stability of the formulation during storage. These differences in pharmaceutical properties together with physicochemical data sug- gest that the pH of the continuous phase used for PEG-NC preparation can modify drug allocation, from the external shell towards the inner lipid core of the nanocapsules. Finally, we tested the bioactivity of the drug-loaded PEG-NC in several tumor cell lines, and also in endothelial cells. The results indicated that drug encapsulation led to an improvement on drug cytotoxicity in tumor cells, but not in non-tumor en- dothelial cells. Altogether, the data confirms that PEG-NC show adequate delivery properties for F10320GD1, and underlines its possible utility as an anticancer therapy.
PB Bentham Science
SN 1873-5294
YR 2014
FD 2014-05
LK http://hdl.handle.net/10347/11294
UL http://hdl.handle.net/10347/11294
LA eng
NO Hervella et al. Curr. Top. Med. Chem. 14, 115-1123, 2014
NO The authors would like to acknowledge financial support from CENIT-NANOFAR XS53 project, FAES Farma S.A. (Spain), Xunta de Galicia (Competitive Reference Ref. GRC2014/043, FEDER Funds) and the European Commission FP7 EraNet — EuroNanoMed Program-Instituto Carlos III (Lymphotarg pro- yect, Ref. PS09/02670). MGF was a recipient of an Isidro Parga Pondal contract.
DS Minerva
RD 24 abr 2026