当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > In situ and in silico evaluation of amine- and folate-terminated dendrimers as nanocarriers of anesthetics.

In situ and in silico evaluation of amine- and folate-terminated dendrimers as nanocarriers of anesthetics.

Abstract：

:The search for new nano-systems for targeted biomedical applications and controlled drug release has attracted significant attention in polymer chemistry, pharmaceutics, and biomaterial science. Controlled drug delivery has many advantages over conventional drug administration, such as reduction of side effects, maintaining a stable plasma level concentration and improving the quality of life of patients. In this study, PAMAM G5 dendrimers and PAMAM G5-folic acid conjugates (PAMAM G5-FA) are synthesized and characterized by mass spectrometry (MALDI-MS). Controlled release studies at different pH values show that PAMAM G5-FA is a good candidate as a carrier for tramadol and morphine, while mathematical modeling is conducted, suggesting that the release process is governed by a diffusion mechanism. In addition, using molecular dynamics simulations, we investigate the structural and energetic properties that facilitate the encapsulation of tramadol and morphine by unmodified and functionalized PAMAM-G5 dendrimers at low, neutral and high pH. Our results correlate well with experimental data, confirming that tramadol and morphine may be encapsulated both by functionalized PAMAM dendrimers and unmodified PAMAM. Moreover, the simulations further reveal that hydrogen-bond and electrostatic interactions govern the affinity the dendrimers for both drugs. This information is envisioned to prove useful for the encapsulation of other drugs and for the design of novel functionalized dendrimers.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Carrasco-Sánchez V,Vergara-Jaque A,Zuñiga M,Comer J,John A,Nachtigall FM,Valdes O,Duran-Lara EF,Sandoval C,Santos LS

doi

10.1016/j.ejmech.2013.11.040

subject

Has Abstract

pub_date

2014-02-12 00:00:00

pages

250-7

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00783-6

journal_volume

73

pub_type

杂志文章

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