External electrostatic interaction versus internal encapsulation between cationic dendrimers and negatively charged drugs: Which contributes more to solubility enhancement of the drugs?

Yiyun Cheng; Qinglin Wu; Yiwen Li; Tongwen Xu

doi:10.1021/jp801742t

External electrostatic interaction versus internal encapsulation between cationic dendrimers and negatively charged drugs: Which contributes more to solubility enhancement of the drugs?

Yiyun Cheng^*
, Qinglin Wu
, Yiwen Li
, Tongwen Xu

^*Corresponding author for this work

University of Science and Technology of China

Research output: Contribution to journal › Article › peer-review

97 Scopus citations

Abstract

Relationships of electrostatic interaction and encapsulation between poly(amidoamine) (PAMAM) dendrimers and negatively charged drug molecules have been investigated by aqueous solubility and NMR (¹H NMR and two-dimensional nuclear Overhauser effect spectroscopy (2D-NOESY)) studies. PAMAM dendrimers significantly increased the solubilities of phenobarbital and sulfamethoxazole, but scarcely influenced those of primidone and trimethoprim. Moreover, ¹H NMR and 2D-NOESY measurements indicated that few phenobarbital or sulfamethoxazole molecules were entrapped in the cavities of low-generation dendrimers (generation 3, G3). These results suggest that external electrostatic interaction contributes more to the solubility enhancement of drugs than internal encapsulation.

Original language	English
Pages (from-to)	8884-8890
Number of pages	7
Journal	Journal of Physical Chemistry B
Volume	112
Issue number	30
DOIs	https://doi.org/10.1021/jp801742t
State	Published - 31 Jul 2008
Externally published	Yes

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10.1021/jp801742t

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title = "External electrostatic interaction versus internal encapsulation between cationic dendrimers and negatively charged drugs: Which contributes more to solubility enhancement of the drugs?",

abstract = "Relationships of electrostatic interaction and encapsulation between poly(amidoamine) (PAMAM) dendrimers and negatively charged drug molecules have been investigated by aqueous solubility and NMR (1H NMR and two-dimensional nuclear Overhauser effect spectroscopy (2D-NOESY)) studies. PAMAM dendrimers significantly increased the solubilities of phenobarbital and sulfamethoxazole, but scarcely influenced those of primidone and trimethoprim. Moreover, 1H NMR and 2D-NOESY measurements indicated that few phenobarbital or sulfamethoxazole molecules were entrapped in the cavities of low-generation dendrimers (generation 3, G3). These results suggest that external electrostatic interaction contributes more to the solubility enhancement of drugs than internal encapsulation.",

author = "Yiyun Cheng and Qinglin Wu and Yiwen Li and Tongwen Xu",

year = "2008",

month = jul,

day = "31",

doi = "10.1021/jp801742t",

language = "英语",

volume = "112",

pages = "8884--8890",

journal = "Journal of Physical Chemistry B",

issn = "1520-6106",

publisher = "American Chemical Society",

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}

External electrostatic interaction versus internal encapsulation between cationic dendrimers and negatively charged drugs: Which contributes more to solubility enhancement of the drugs? / Cheng, Yiyun; Wu, Qinglin; Li, Yiwen et al.
In: Journal of Physical Chemistry B, Vol. 112, No. 30, 31.07.2008, p. 8884-8890.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - External electrostatic interaction versus internal encapsulation between cationic dendrimers and negatively charged drugs

T2 - Which contributes more to solubility enhancement of the drugs?

AU - Cheng, Yiyun

AU - Wu, Qinglin

AU - Li, Yiwen

AU - Xu, Tongwen

PY - 2008/7/31

Y1 - 2008/7/31

N2 - Relationships of electrostatic interaction and encapsulation between poly(amidoamine) (PAMAM) dendrimers and negatively charged drug molecules have been investigated by aqueous solubility and NMR (1H NMR and two-dimensional nuclear Overhauser effect spectroscopy (2D-NOESY)) studies. PAMAM dendrimers significantly increased the solubilities of phenobarbital and sulfamethoxazole, but scarcely influenced those of primidone and trimethoprim. Moreover, 1H NMR and 2D-NOESY measurements indicated that few phenobarbital or sulfamethoxazole molecules were entrapped in the cavities of low-generation dendrimers (generation 3, G3). These results suggest that external electrostatic interaction contributes more to the solubility enhancement of drugs than internal encapsulation.

AB - Relationships of electrostatic interaction and encapsulation between poly(amidoamine) (PAMAM) dendrimers and negatively charged drug molecules have been investigated by aqueous solubility and NMR (1H NMR and two-dimensional nuclear Overhauser effect spectroscopy (2D-NOESY)) studies. PAMAM dendrimers significantly increased the solubilities of phenobarbital and sulfamethoxazole, but scarcely influenced those of primidone and trimethoprim. Moreover, 1H NMR and 2D-NOESY measurements indicated that few phenobarbital or sulfamethoxazole molecules were entrapped in the cavities of low-generation dendrimers (generation 3, G3). These results suggest that external electrostatic interaction contributes more to the solubility enhancement of drugs than internal encapsulation.

UR - https://www.scopus.com/pages/publications/49349117727

U2 - 10.1021/jp801742t

DO - 10.1021/jp801742t

M3 - 文章

AN - SCOPUS:49349117727

SN - 1520-6106

VL - 112

SP - 8884

EP - 8890

JO - Journal of Physical Chemistry B

JF - Journal of Physical Chemistry B

IS - 30

ER -

External electrostatic interaction versus internal encapsulation between cationic dendrimers and negatively charged drugs: Which contributes more to solubility enhancement of the drugs?

Abstract

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