Topical drug delivery by a polymeric nanosphere gel: Formulation optimization and in vitro and in vivo skin distribution studies

Batheja, Priya; Sheihet, Larisa; Kohn, Joachim; Singer, Adam J.; Michniak‐Kohn, Bozena

doi:10.1016/j.jconrel.2010.10.005

Cited by 174 publications

(112 citation statements)

References 48 publications

Supporting

Mentioning

101

Contrasting

Order By: Relevance

“…19,20 The effects of drug loading on the skin permeation of schaftoside and isoschaftoside were also investigated. The cumulative amounts of schaftoside and isoschaftoside crossing the skin increased with increased drug loading ( Figure 6).…”

Section: In Vitro Skin Permeationmentioning

confidence: 99%

Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis

Shen

Zhang

Wang

et al. 2014

IJN

View full text Add to dashboard Cite

The aims of the present study were to investigate the skin permeation and cellular uptake of a microemulsion (ME) containing total flavone of rhizoma arisaematis (TFRA), and to evaluate its effects on skin structure. Pseudo-ternary phase diagrams were constructed to evaluate ME regions with various surfactants and cosurfactants. Eight formulations of oil-in-water MEs were selected as vehicles, and in vitro skin-permeation experiments were performed to optimize the ME formulation and to evaluate its permeability, in comparison to that of an aqueous suspension. Laser scanning confocal microscopy and fluorescent-activated cell sorting were used to explore the cellular uptake of rhodamine 110-labeled ME in human epidermal keratinocytes (HaCaT) and human embryonic skin fibroblasts (CCC-ESF-1). The structure of stratum corneum treated with ME was observed using a scanning electron microscope. Furthermore, skin irritation was tested to evaluate the safety of ME. ME formulated with 4% ethyl oleate (weight/weight), 18% Cremophor EL ® (weight/weight), and 18% Transcutol ® P, with 1% Azone to enhance permeation, showed good skin permeability. ME-associated transdermal fluxes of schaftoside and isoschaftoside, two major effective constituents of TFRA, were 3.72-fold and 5.92-fold higher, respectively, than those achieved using aqueous suspensions. In contrast, in vitro studies revealed that uptake by HaCaT and CCC-ESF-1 cells was lower with ME than with an aqueous suspension. Stratum corneum loosening and shedding was observed in nude mouse skin treated with ME, although ME produced no observable skin irritation in rabbits. These findings indicated that ME enhanced transdermal TFRA delivery effectively and showed good biocompatibility with skin tissue.

show abstract

Section: In Vitro Skin Permeationmentioning

confidence: 99%

Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis

Shen

Zhang

Wang

et al. 2014

IJN

View full text Add to dashboard Cite

show abstract

“…42 Cutaneous penetration of free and nanoencapsulated Hst was determined from successive tape stripping of the stratum corneum and extraction of the drug from the skin layers. Our results (Figure 4) showed significantly higher quantities (P,0.05) of Hst from LNC-Hst (6.31±0.10 µg/cm 2 ) than from free-Hst (5.52±0.21 µg/cm 2 ) in the stratum corneum.…”

mentioning

confidence: 99%

Hesperetin-loaded lipid-core nanocapsules in polyamide: a new textile formulation for topical drug delivery

Menezes

Frank

Lima

et al. 2017

IJN

View full text Add to dashboard Cite

Chronic venous insufficiency is characterized by chronic reflux disorder of blood from the peripheral to the central vein, with subsequent venous hypertension and resulting changes in the skin. Traditionally, nonsurgical treatments relied on the use of compression therapy, and more recently a variety of flavonoids have been shown to have positive effects. There have also been developments of more effective drug delivery systems using various textiles and nanotechnology to provide new therapeutic options. Our objective was to use nanotechnology to develop a new formulation containing hesperetin (Hst), a substance not previously used in the treatment of chronic venous insufficiency, impregnated into textile fibers as a possible alternative treatment of venous diseases. We prepared the nanocapsules using the interfacial deposition of preformed polymer method with an Hst concentration of 0.5 mg/mL and then characterized the size and distribution of particles. To quantify the Hst in the samples, we developed an analytical method using high-performance liquid chromatography. Studies of encapsulation efficiency (98.81%±0.28%), microscopy, drug release (free-Hst: 104.96%±12.83%; lipid-core nanocapsule-Hst: 69.90%±1.33%), penetration/permeation, drug content (0.46±0.01 mg/mL) and the effect of washing the textile after drug impregnation were performed as part of the study. The results showed that nanoparticles of a suitable size and distribution with controlled release of the drug and penetration/permeation into the skin layers were achieved. Furthermore, it was established that polyamide was able to hold more of the drug, with a 2.54 times higher content than the cotton fiber; after one wash and after five washes, this relation was 2.80 times higher. In conclusion, this is a promising therapeutic alternative to be further studied in clinical trials.

show abstract

“…PG:water was chosen as a base solvent on account of its ability to solubilize most tested components, including Z. bungeanum oil and Azone. Moreover, as the well-established and standard penetration enhancer, Azone had been employed by many researchers to achieve significant permeation enhancement and the concentration (0.2 mol/L) was typically used in skin penetration enhancement studies (Meidan et al, 2003;Kaushik et al, 2010;Batheja et al, 2011); hence 0.2 mol/L Azone was used to compare and better evaluate the permeation enhancement activity of the oil.…”

Section: Effects Of Z Bungeanum Oil On Percutaneous Permeation Of Momentioning

confidence: 99%

Cytotoxicity and enhancement activity of essential oil from Zanthoxylum bungeanum Maxim. as a natural transdermal penetration enhancer

Mao

et al. 2014

J. Zhejiang Univ. Sci. B

View full text Add to dashboard Cite

Abstract:The aim of this present study is to investigate the effect of Zanthoxylum bungeanum oil (essential oil from Z. bungeanum Maxim.) on cytotoxicity and the transdermal permeation of 5-fluorouracil and indomethacin. The cytotoxicity of Z. bungeanum oil on dermal fibroblasts and epidermal keratinocytes was studied using an MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The rat skin was employed to determine the percutaneous penetration enhancement effect of Z. bungeanum oil on hydrophilic and lipophilic model drugs, i.e., 5-fluorouracil and indomethacin. The secondary structure changes of the rat stratum corneum (SC) were determined using attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), and saturated solubilities and SC/vehicle partition coefficients of two model drugs with and without Z. bungeanum oil were also measured to understand its related mechanisms of action. It was found that the half maximal inhibitory concentration (IC 50 ) values of Z. bungeanum oil were significantly lower in HaCaT and CCC-ESF-1 cell lines compared to the well-established and standard penetration enhancer Azone. The Z. bungeanum oil at various concentrations effectively facilitated the percutaneous penetration of two model drugs across the rat skin. In addition, the mechanisms of permeation enhancement by Z. bungeanum oil could be explained with saturated solubility, SC/vehicle partition coefficient, and secondary structure changes of SC.

show abstract

Topical drug delivery by a polymeric nanosphere gel: Formulation optimization and in vitro and in vivo skin distribution studies

Cited by 174 publications

References 48 publications

Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis

Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis

Hesperetin-loaded lipid-core nanocapsules in polyamide: a new textile formulation for topical drug delivery

Cytotoxicity and enhancement activity of essential oil from Zanthoxylum bungeanum Maxim. as a natural transdermal penetration enhancer

Contact Info

Product

Resources

About