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dc.contributor.authorHervella, Pablo
dc.contributor.authorAlonso-Sande, Maria
dc.contributor.authorLedo, Francisco
dc.contributor.authorLucero, Maria L.
dc.contributor.authorAlonso Fernández, María José
dc.contributor.authorGarcía-Fuentes, Marcos
dc.date.accessioned2014-08-18T08:29:44Z
dc.date.available2014-08-18T08:29:44Z
dc.date.issued2014-05
dc.identifier.citationHervella et al. Curr. Top. Med. Chem. 14, 115-1123, 2014
dc.identifier.issn1873-5294
dc.identifier.urihttp://hdl.handle.net/10347/11294
dc.description.abstractDrugs 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.
dc.description.sponsorshipThe 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.
dc.language.isoeng
dc.publisherBentham Science
dc.subjectNanomedicine
dc.subjectNanocapsules
dc.subjectTargeting
dc.subjectCancer therapy
dc.subjectEncapsulation
dc.subjectControlled release
dc.subject.classificationMaterias::Investigación::33 Ciencias tecnológicas::3314 Tecnología médica
dc.titlePegylated lipid nanocapsules with improved drug encapsulation and controlled release properties
dc.typepreprint
dc.identifier.doi10.2174/1568026614666140329224716
dc.relation.publisherversionhttp://dx.doi.org/10.2174/1568026614666140329224716
dc.rights.accessRightsopen access


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