Poly(amidoamine) dendrimers as skin penetration enhancers: Influence of charge, generation, and concentration

Venuganti, Venkata Vamsi Krishna; Perumal, Omathanu

doi:10.1002/jps.21603

Cited by 129 publications

(79 citation statements)

References 39 publications

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“…18 The application of dendrimers as topical enhancers for transdermal drug delivery also has been considered, as modified PAMAM dendrimers can significantly improve the transdermal bioavailability of compounds such as nonsteroidal anti-inflammatory drugs and antiarthritic and anticancer drugs, which often cause gastrointestinal adverse effects. [20][21][22] Some hyperproliferative skin disorders, such as psoriasis and atopic eczema, are treated by photochemotherapy with oral psoralens such as a combination of 8-methoxypsoralene (8-MOP) and ultraviolet A radiation (PUVA therapy). Oral or topical administration of 8-MOP causes many adverse effects.…”

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confidence: 99%

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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confidence: 99%

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

Uram

Szuster

Gargasz

et al. 2013

IJN

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“…For PAMAM dendrimers with different surface charge, the enhancement effect was in the following decreasing order: G4-NH 2 4G4-OH4G3.5-COOH. Transepidermal water loss, skin resistance measurement and ATR-FTIR studies revealed that the cationic dendrimers could more easily interact with the SC lipids and influence drug permeation through the skin (Venuganti & Perumal, 2009). In another study, Filipowicz et al (2011) also reported that the small-sized G2-NH 2 dendrimer might be a more potent penetration enhancer than the larger ones for the transdermal absorption of the hydrophilic drug (riboflavin) from the emulsions or hydrogels.…”

Section: Dendrimersmentioning

confidence: 97%

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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“…However, many new drugs are hydrophobic causing low water-solubility that results in insufficient levels of drug delivered into cells. Water soluble and biocompatible dendritic species are known to improve drug solubility and plasma circulation time via transdermal formulations and to deliver drugs quickly and effectively [72,[76][77][78][79][80][81]. In this regard, dendrimers have been shown to be useful as transdermal drug delivery systems for various types of medications [77,80,81], including anticancer, antiviral, nonsteroidal anti-inflammatory and antihypertensive drugs.…”

Section: Transdermal Drug Deliverymentioning

confidence: 99%

Polyester Dendrimers: Smart Carriers for Drug Delivery

Twibanire

Grindley

2014

Polymers

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Polyester dendrimers have been shown to be outstanding candidates for biomedical applications. Compared to traditional polymeric drug vehicles, these biodegradable dendrimers show excellent advantages especially as drug delivery systems because they are non-toxic. Here, advances on polyester dendrimers as smart carriers for drug delivery applications have been surveyed. Both covalent and non-covalent incorporation of drugs are discussed.

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Poly(amidoamine) dendrimers as skin penetration enhancers: Influence of charge, generation, and concentration

Cited by 129 publications

References 39 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

Polyester Dendrimers: Smart Carriers for Drug Delivery

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Poly(amidoamine) dendrimers as skin penetration enhancers: Influence of charge, generation, and concentration

Cited by 129 publications

References 39 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

Polyester Dendrimers: Smart Carriers for Drug Delivery

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Product

Resources

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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