Mechanism of enhancement effect of dendrimer on transdermal drug permeation through polyhydroxyalkanoate matrix

Wang, Zhixiong; Itoh, Yoshiaki; Hosaka, Yoshifumi; Kobayashi, Ichiro; Nakano, Yoshihisa; Maeda, Isamu; Umeda, Fusako; Yamakawa, Junji; Nishimine, Mari; Suenobu, Tomoyoshi; Fukuzumi, Shunichi; Kawase, Masaya; Yagi, Kiyohito

doi:10.1016/s1389-1723(04)70146-2

Cited by 44 publications

(10 citation statements)

References 16 publications

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“…It has been proven, however, that full-generation G3 and G4 PAMAM dendrimers may serve as useful carriers for 8-MOP, increasing its permeability, as evidenced in vitro and in vivo. [23][24][25] The enhancement of transdermal delivery of tamsulosin, 26 as well as the promotion of the transdermal diffusion of riboflavin by G2-G5 PAMAM, 27 were also shown.…”

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confidence: 88%

In vitro cytotoxicity of the ternary PAMAM G3–pyridoxal–biotin bioconjugate

Uram

Szuster

Gargasz

et al. 2013

IJN

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A third-generation polyamidoamine dendrimer (PAMAM G3) was used as a macromolecular carrier for pyridoxal and biotin. The binary covalent bioconjugate of G3, with nine molecules of biotin per one molecule of G3 (G3 9B ), and the ternary covalent bioconjugate of G3, with nine biotin and ten pyridoxal molecules (G3 9B10P ), were synthesized. The biotin and pyridoxal residues of the bioconjugate were available for carboxylase and transaminase enzymes, as demonstrated in the conversion of pyruvate to oxaloacetate and alanine to pyruvate, respectively, by in vitro monitoring of the reactions, using 1 H nuclear magnetic resonance spectroscopy. The toxicity of the ternary bioconjugate (BC-PAMAM) was studied in vitro on BJ human normal skin fibroblasts and human squamous cell carcinoma (SCC-15) cell cultures in comparison with PAMAM G3, using three cytotoxicity assays (XTT, neutral red, and crystal violet) and an estimation of apoptosis by confocal microscopy detection. The tests have shown that BC-PAMAM has significantly lower cytotoxicity compared with PAMAM. Nonconjugated PAMAM was not cytotoxic at concentrations up to 5 μM (NR) and 10 μM (XTT), and BC-PAMAM was not cytotoxic up to 50 μM (both assays) for both cell lines. It has been also found that normal fibroblasts were more sensitive than SCC to both PAMAM and BC-PAMAM. The effect of PAMAM and BC-PAMAM on the initiation of apoptosis (PAMAM in fibroblasts at 5 μM and BC-PAMAM at 10 μM in both cell lines) corresponded with cytotoxicity assays for both cell lines. We concluded that normal fibroblasts are more sensitive to the cytotoxic effects of the PAMAM G3 dendrimer and that modification of its surface cationic groups by substitution with biologically active molecules significantly decreases that effect, confirming that PAMAM G3 is a useful candidate as a carrier for active biocompound delivery.

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mentioning

confidence: 88%

In vitro cytotoxicity of the ternary PAMAM G3–pyridoxal–biotin bioconjugate

Uram

Szuster

Gargasz

et al. 2013

IJN

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“…Further mechanistic study revealed that tamsulosin crystals had highly ordered orientation in the dendrimer-PHA matrix, which could limit the diffusion direction of tamsulosin and facilitate the drug permeation through the skin (Wang et al, 2003b). Cheng et al (2007) suggested that PAMAM dendrimer (G5-NH 2 ) could covalently conjugate with different NSAIDs (ketoprofen or diflunisal), significantly improve the drug permeation through the skin and achieve a prolonged pharmcodynamic profile.…”

Section: Dendrimersmentioning

confidence: 99%

Biomaterials as novel penetration enhancers for transdermal and dermal drug delivery systems

2013

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The highly organized structure of the stratum corneum provides an effective barrier to the drug delivery into or across the skin. To overcome this barrier function, penetration enhancers are always used in the transdermal and dermal drug delivery systems. However, the conventional chemical enhancers are often limited by their inability to delivery large and hydrophilic molecules, and few to date have been routinely incorporated into the transdermal formulations due to their incompatibility and local irritation issues. Therefore, there has been a search for the compounds that exhibit broad enhancing activity for more drugs without producing much irritation. More recently, the use of biomaterials has emerged as a novel method to increase the skin permeability. In this paper, we present an overview of the investigations on the feasibility and application of biomaterials as penetration enhancers for transdermal or dermal drug delivery systems.

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“…Being there in PHA matrix, nanorobots persuade decidedly ordered orientation of tamsulosin crystals, which promoted drug release. Attributed to restricted dissemination direction, tamsulosin diffusion was facilitated through snake skin39.…”

Section: Dendrimer Mediated Transdermal Drug Deliverymentioning

confidence: 99%

Dendrimeric nanoarchitectures mediated transdermal and oral delivery of bioactives

et al. 2008

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Transdermal route is an evolving panorama in novel drug deliverance and with oral route they proffer immense potential. Most recently there is hastening in approaches for delivering bioactives via these routes, amongst them revolution has been made by dendrimers. Encapsulation and conjugation of bioactives with these virus sized robots have shown immense employment for delivery of hydrophobic and labile remedies. Transport of these nano-cruises from corner to corner of skin and through epithelial hurdle of gastrointestinal tract depends upon dendrimer characteristics. An improved thoughtful of these characteristics is an obligation for their use in these rambling fields. These characteristics embrace generation size, molecular weight, surface charge, incubation time and concentration. This context demarcates the imperative role of dendrimers in transdermal and oral drug delivery. This review also highlights concerning mechanism of convey of nanoarrays via epithelial hurdle of GIT.

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Mechanism of enhancement effect of dendrimer on transdermal drug permeation through polyhydroxyalkanoate matrix

Cited by 44 publications

References 16 publications

In vitro cytotoxicity of the ternary PAMAM G3–pyridoxal–biotin bioconjugate

In vitro cytotoxicity of the ternary PAMAM G3–pyridoxal–biotin bioconjugate

Biomaterials as novel penetration enhancers for transdermal and dermal drug delivery systems

Dendrimeric nanoarchitectures mediated transdermal and oral delivery of bioactives

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Mechanism of enhancement effect of dendrimer on transdermal drug permeation through polyhydroxyalkanoate matrix

Cited by 44 publications

References 16 publications

In vitro cytotoxicity of the ternary PAMAM G3&ndash;pyridoxal&ndash;biotin bioconjugate

In vitro cytotoxicity of the ternary PAMAM G3&ndash;pyridoxal&ndash;biotin bioconjugate

Biomaterials as novel penetration enhancers for transdermal and dermal drug delivery systems

Dendrimeric nanoarchitectures mediated transdermal and oral delivery of bioactives

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Product

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In vitro cytotoxicity of the ternary PAMAM G3–pyridoxal–biotin bioconjugate

In vitro cytotoxicity of the ternary PAMAM G3–pyridoxal–biotin bioconjugate