Enhancing effect of modified beta-cyclodextrins on in vitro skin permeation of estradiol

Paula, Daniel de; Oliveira, Dionéia Camilo Rodrigues de; Tedesco, Antônio Cláudio; Bentley, Maria Vitória Lopes Badra

doi:10.1590/s1516-93322007000100014

Cited by 8 publications

(11 citation statements)

References 27 publications

(41 reference statements)

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“…The emulsion containing the HPβCD-entrapped extract was stored in a well-closed glass container at an accelerated temperature, 45.0 ± 2.0°C for www.scienceasia.org 90 days 29 . The physical characteristics including droplet size, viscosity, and pH at before and after stability test under storage condition were determined.…”

Section: Stability Studymentioning

confidence: 99%

“…The skin tissue was mounted on the receptor compartment with the epidermal side facing upward into the donor compartment. The temperature of the receptor medium was set at 37°C, and the skin temperature was controlled at 32 ± 1°C as described previously 29,30 . One hundred milligrams of the emulsion containing the HPβCD-entrapped extract or the unentrapped extract were evenly spread on the surface of stratum corneum (st. corneum), outermost layer of epidermis.…”

Section: In Vitro Permeation Studymentioning

confidence: 99%

“…DSC was used to confirm the interaction between the extract and HPβCD molecule. The principle of this method is when the extract is entrapped in an HPβCD cavity or interacts with HPβCD, its melting point changes to a different temperature or disappears 29 . Fig.…”

Section: Physical Characteristics Of the Hpβcd-entrapped Extractmentioning

confidence: 99%

“…Generally, the partition of a given compound depends not only on the st. corneum concentration but also on its solubility in a more hydrophilic deeper layer 29,36 . In the present study, there was no difference in amount of saponins accumulated in the viable layer between skin applied with emulsions with and without the entrapped extract.…”

Section: The Permeation Of Saponins Through the Skinmentioning

confidence: 99%

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Stability and clinical effectiveness of emulsion containing Asparagus racemosus root extract

Rungsang¹,

Tuntijarukorn²,

Ingkaninan³

et al. 2015

ScienceAsia

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Asparagus racemosus root extract was entrapped in hydroxypropyl-β-cyclodextrin (HPβCD) by a physical mixing method and then incorporated in an oil in water (o/w) emulsion to evaluate its stability and clinical effectiveness. After the emulsion containing the HPβCD-entrapped extract was kept at 45.0 ± 2.0°C for 90 days, 90% of saponins, major compounds of the extract, remained. Without entrapment with HPβCD, the amount of saponins would have decreased to 10% after storage for 60 days. After application of the emulsion containing the entrapped extract or the unentrapped extract to the outermost layer of full thickness skin, about 38% of saponins could penetrate into the skin. A higher amount of saponins was accumulated in the outermost layer applied with emulsion containing the entrapped extract. For a clinical study, measurement of the surface evaluation of wrinkles (SEw) at the zygomatic area of the face was measured at weeks 8 and 12. The average SEw value of group of subjects that applied the extract-free emulsion was significantly higher than that of the group that applied the emulsion containing the entrapped extract (p < 0.05). Our study indicates that in o/w emulsion, saponins in A. racemosus root extract could maintain their stability after entrapping the extract within HPβCD. Moreover, the effectiveness of the entrapped extract on prevention of wrinkle progression was seen.

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Section: Stability Studymentioning

confidence: 99%

Section: In Vitro Permeation Studymentioning

confidence: 99%

Section: Physical Characteristics Of the Hpβcd-entrapped Extractmentioning

confidence: 99%

Section: The Permeation Of Saponins Through the Skinmentioning

confidence: 99%

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Stability and clinical effectiveness of emulsion containing Asparagus racemosus root extract

Rungsang¹,

Tuntijarukorn²,

Ingkaninan³

et al. 2015

ScienceAsia

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“…Hampered aqueous solubility of native β-CD had given advantage for chemical modification by substitution with alkyl groups like methyl, hydroxypropyl and sulfobutyl ether resulting in enormous amplification in solubility with good safety profile [8]. Modified β-CD have gained wider applications in delivering the drugs (BCS class II and IV) via different routes of administration due to their increased solubilizing effect resulting in stable inclusion complexes and improved permeation across biological membranes [9,10].…”

Section: Introductionmentioning

confidence: 99%

Enhanced Dissolution Efficiency of Zaleplon Solid Dispersions via Modified β-Cyclodextrin Molecular Inclusion Complexes

Popescu¹

2015

J.Pharm Pharm Scien

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The focus of the current study is to confirm the potential of chemically modified cyclodextrins (methyl-β-cyclodextrin (MβCD/Kleptose® Crysmeb), hydroxypropyl-β-cyclodextrin (HP-β-CD/Kleptose® HPB) and sulfobutylether-β-cyclodextrin (SBE-β-CD/Captisol®)) to improve the dissolution rate of zaleplon in oral delivery. Native and modified cyclodextrins were screened via phase solubility studies in order to select the most efficient cyclodextrin in formation of stable inclusion complexes. A L -type phase solubilization resulted from phase solubility diagrams of all cyclodextrin indicated a linear proportional relation between the solubility of zaleplon versus different CD concentrations. Complexation with crysmeb and HP-β-CD resulted in greater complexation constant values and higher percentage complexation efficiency values. Therefore these two cyclodextrins were selected for formulation development. Inclusion complexes of zaleplon:cyclodextrin solid dispersions were prepared using lyophilization and spray-drying techniques. DSC and XRD performance delineates the transformation of crystalline form of zaleplon to amorphous state. 1 HNMR studies confirm the presence of drug in the hydrophobic cavity of cyclodextrins and reveal the amorphous nature of the formulations. The stability studies of inclusion complexes for 60 days at 25°C/60 % RH and 40°C/75%RH resulted in low or no variations in the percentage of complexation efficiency suggesting good stability of molecular complexes. In conclusion, in vitro dissolution studies displayed an overall two-fold improvement in the dissolution rate compared to pure drug attributed to Crysmeb and HP-β-CD as suitable complexing agents in enhancing the solubility of zaleplon.

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Cyclodextrin-Steroid Interactions and Applications to Pharmaceuticals, Food, Biotechnology and Environment

Fenyvesi

Puskás

Szente

2018

Environmental Chemistry for a Sustainable World

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Enhancing effect of modified beta-cyclodextrins on in vitro skin permeation of estradiol

Abstract: Estradiol, the most important hormone in females, was complexed with hydroxypropyl-β-cyclodextrin (HP-β-CD) and randomly methylated β-cyclodextrin (RM-β-CD

Cited by 8 publications

References 27 publications

Stability and clinical effectiveness of emulsion containing Asparagus racemosus root extract

Stability and clinical effectiveness of emulsion containing Asparagus racemosus root extract

Enhanced Dissolution Efficiency of Zaleplon Solid Dispersions via Modified β-Cyclodextrin Molecular Inclusion Complexes

Cyclodextrin-Steroid Interactions and Applications to Pharmaceuticals, Food, Biotechnology and Environment

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