Development of Poly(lactide-co-glicolide) Nanoparticles Incorporating Morphine Hydrochloride to Prolong its Circulation in Blood

Author(s): Victoria Gomez-Murcia, Mercedes Garcia Montalban, Juan C. Gomez-Fernandez*, Pilar Almela

Journal Name: Current Pharmaceutical Design

Volume 23 , Issue 13 , 2017


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Abstract:

Background: Formulations incorporating nanoparticles (NPs) are widely used to prolong drug release. In this regard, poly(lactide-co-glicolide) (PLGA) is often used in their preparation due to its high degree of biocompatibility and biodegradability. In the present study, morphine HCl is incorporated in PLGA-NPs and different preparation alternatives are evaluated for their effects on the properties, stability and capacity of encapsulation.

Methods: NPs were prepared by a double emulsion solvent diffusion-ammonium loading (DESD-AL) or double emulsion solvent diffusion-traditional (DESD-T) technique. NP morphology, size, zeta potential and encapsulation efficiency were investigated. In vitro studies were performed in phosphate buffer pH 7.4 at 37 ºC and deionized water at 4ºC. Adult male Swiss mice were used to study the pharmacokinetic behavior in vivo.

Results: Our results show that DESD-AL provides a higher level of morphine entrapment and that increasing the sonication time reduces the size but does not appreciably reduce the entrapment percentage. It was also observed that NP stability was greater when Pluronic F68 was used rather than PVA, and that in vitro assays provided better results with low concentrations of both stabilizers. Lyophilized NPs, after rehydration showed properties that were only slightly different from those of the untreated ones, with no sign of precipitation or aggregation. Finally, the obtained NPs enhanced morphine bioavailability.

Conclusions: In conclusion, a useful method for encapsulating morphine in order to obtain an extended delivery period is described and its effects are compared with those of the free drug.

Keywords: Morphine, nanoparticles, PLGA, pharmacokinetics, lyophilized, poly(lactide-co-glicolide) (PLGA).

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Article Details

VOLUME: 23
ISSUE: 13
Year: 2017
Published on: 23 May, 2017
Page: [2015 - 2025]
Pages: 11
DOI: 10.2174/1381612822666161201152604
Price: $65

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