Sonophoresis‐mediated permeation and retention of peptide dendrimers across human epidermis

Mutalik, Srinivas; Nayak, Usha Y.; Kalra, Rohit; Kumar, Aravind; Kulkarni, Raghavendra V.; Parekh, Harendra S.

doi:10.1111/j.1600-0846.2011.00539.x

Cited by 29 publications

(17 citation statements)

References 26 publications

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“…The skin was wiped dry, scissor-cut into small pieces and homogenized with 5 mL of phosphate buffer pH 6.8. The resultant mixture was passed through a 0.45 mm membrane and the filtrate was analyzed for EGCG using HPLC (Mutalik et al, 2012;Mutalik et al, 2014).…”

Section: Expression Of Mmp-2 and Mmp-9 By Gelatin Zymographymentioning

confidence: 99%

Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage

et al. 2017

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(2017) Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage, Drug Delivery, 24:1, 61-74, DOI: 10.1080/10717544.2016 AbstractThe present work attempts to develop and statistically optimize transfersomes containing EGCG and hyaluronic acid to synergize the UV radiation-protective ability of both compounds, along with imparting antioxidant and anti-aging effects. Transfersomes were prepared by thin film hydration technique, using soy phosphatidylcholine and sodium cholate, combined with high-pressure homogenization. They were characterized with respect to size, polydispersity index, zeta potential, morphology, entrapment efficiency, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD), in vitro antioxidant activity and ex vivo skin permeation studies. Cell viability, lipid peroxidation, intracellular ROS levels and expression of MMPs (2 and 9) were determined in human keratinocyte cell lines (HaCaT). The composition of the transfersomes was statistically optimized by Design of Experiments using Box-Behnken design with four factors at three levels. The optimized transfersome formulation showed vesicle size, polydispersity index and zeta potential of 101.2 ± 6.0 nm, 0.245 ± 0.069 and À44.8 ± 5.24 mV, respectively. FTIR and DSC showed no interaction between EGCG and the selected excipients. XRD results revealed no form conversion of EGCG in its transfersomal form. The optimized transfersomes were found to increase the cell viability and reduce the lipid peroxidation, intracellular ROS and expression of MMPs in HaCaT cells. The optimized transfersomal formulation of EGCG and HA exhibited considerably higher skin permeation and deposition of EGCG than that observed with plain EGCG. The results underline the potential application of the developed transfersomes in sunscreen cream/lotions for improvement of UV radiation-protection along with deriving antioxidant and anti-aging effects.

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Section: Expression Of Mmp-2 and Mmp-9 By Gelatin Zymographymentioning

confidence: 99%

Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage

et al. 2017

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“…The studies in the presence of dendrimers were conducted either by (i) simultaneously application of drug and dendrimer or (ii) pretreating skin with dendrimers 2 h prior to application of drug solution (Mutalik et al, 2012).…”

Section: Skin Permeation Studies In Presence Of Peptide Dendrimersmentioning

confidence: 99%

Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers

et al. 2013

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Enhancing the deposition and permeation of 5-fluorouracil across human epidermis assisted by appropriately charged and well-defined peptide dendrimers was investigated. Peptide dendrimers with arginine as the terminal amino acid and having a range of terminal positive charges (4þ and 16 þ ) were synthesized by solid phase peptide synthesis. Various parameters including effect of peptide dendrimers on the solubility and partition coefficient of 5-FU, degradation of drug in skin as well as deposition and permeation of 5-FU in/through skin were studied. All the tested dendrimers increased the aqueous solubility and partition coefficient of 5-FU with each also significantly (p50.05) enhancing the deposition and permeation of 5-FU in/across human epidermis in a concentration-dependent manner. Of the three peptide dendrimers examined, R8 dendrimer (bearing 8 þ charge derived from four terminal arginines and MW of &1000 Da) showed greatest values for flux, Q 48 (cumulative amount of drug permeated at the end of 48 h) and amount of drug retained in human skin. Furthermore, this study also scrutinized and reports on the likely mechanisms by which peptide dendrimers act as transdermal permeation enhancers.

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“…Peptide dendrimers are radial or wedge-like macromolecules comprising various basic amino acids linked via peptide/amide bonds which are present both within the branching core and on their outer surface [22,23]. To this end, no reports are available on the application of peptide dendrimers in transdermal drug delivery, except those published exclusively from our group [24,25]. With respect to transdermal delivery and peptide dendrimers, we recently reported the successful application of ultrasound on the permeation of synthesized peptide dendrimers across human skin [24,26].…”

Section: Introductionmentioning

confidence: 99%

Iontophoresis-Mediated Transdermal Permeation of Peptide Dendrimers across Human Epidermis

Mutalik

Parekh

Anissimov

et al. 2013

Skin Pharmacol Physiol

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Purpose of the Study: The overall aim of the present work was to elucidate the effects of iontophoresis on assisting permeation/deposition of peptide dendrimers across/within human skin. Procedures: A series of peptide dendrimers containing arginine and histidine as terminal acids were synthesized and characterized. These dendrimers were subjected to passive and iontophoretic permeation studies across human epidermis. Results: The synthesized peptide dendrimers were found to be stable in epidermal, dermal and skin extracts up to 6 h. Passive diffusion studies revealed that none of the synthesized peptide dendrimers permeated human epidermis up to 6 h, although minute concentrations of low molecular weight dendrimers were detected in receptor medium at the end of 24 h. Application of iontophoresis significantly increased the permeation of all the tested peptide dendrimers across human skin in a molecular weight-dependent manner compared to simple passive diffusion. Electromigration was found to be the dominant mechanism behind the iontophoretic permeation of peptide dendrimers across human skin. Conclusions: The present study demonstrates that iontophoresis is an effective technique in enhancing the transdermal permeation of peptide dendrimers. Message of the Paper: This study foresees the possibility of applying peptide dendrimers in iontophoretic delivery of drugs and macromolecules across/within the skin.

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Sonophoresis‐mediated permeation and retention of peptide dendrimers across human epidermis

Abstract: The present study reveals the successful application of sonophoresis in enhancing the permeation of peptide dendrimers across human skin.

Cited by 29 publications

References 26 publications

Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage

Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage

Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers

Iontophoresis-Mediated Transdermal Permeation of Peptide Dendrimers across Human Epidermis

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