Alleviation of prochlorperazine-induced primary irritation of skin by cyclodextrin complexation.

Uekama, Kaneto; Irie, Tetsumi; Sunada, Miki; Otagiri, Masaki; Arimatsu, Yoshiki; Nomura, Shigeru

doi:10.1248/cpb.30.3860

Cited by 36 publications

(12 citation statements)

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“…The possible enhancing mechanisms of CyDs on the bioavailability of drugs in various administration routes are summarized as follows: 1) hydrophilic CyDs increase the solubility, dissolution rate, and wettability of poorly watersoluble drugs, [82][83][84][85][86][87][88][89][90][91][92][93][94][95][96][97][98][99][100][101] 2) CyDs prevent the degradation or disposition of chemically unstable drugs in gastrointestinal tracts as well as during storage, [102][103][104][105][106][107][108][109][110][111] 3) CyDs perturb the membrane fluidity to lower the barrier function, which consequently enhances the absorption of drugs including peptide and protein drugs through the nasal and rectal mucosa, [112][113][114][115][116][117][118][119][120][121] 4) competitive inclusion complexation with third components (bile acid, cholesterol, lipids, etc.) to release the included drug, [122][123][124][1...…”

Section: Enhancement Of Drug Absorption By Hydrophilic Cydsmentioning

confidence: 99%

Design and Evaluation of Cyclodextrin-Based Drug Formulation

2004

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Section: Enhancement Of Drug Absorption By Hydrophilic Cydsmentioning

confidence: 99%

Design and Evaluation of Cyclodextrin-Based Drug Formulation

2004

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“…Uekama et al 109 showed that both γ-CD and -CD were able to lessen the skin irritancy of prochlorperazine while R-CD actually enhanced the irritancy. They concluded that the weak irritancy of γ-CD itself made it more usable than -CD.…”

Section: Cyclodextrins and Site Of Administration Irritationsmentioning

confidence: 99%

“…While these results demonstrate that it is possible to increase transdermal acitretin delivery through the use of RM--CD, it is unclear whether this increase is a result of increased acitretin solubility solely or a combination of increased solubility and membrane permeability due to removal of membrane components by the methylated cyclodextrins. 226,227 Other recent studies on the use of cyclodextrins in topical formulations include a report by Loftsson and Sigurdardót-tir 228 on the effect of poly(vinylpyrrolidone) (PVP) and HMPC in the presence of HP--CD on the flux of hydrocortisone through hairless mouse skin in vitro. In these studies, 1.6% (w/v) suspensions or solutions of hydrocortisone in aqueous HP--CD solution (5-25%) in the presence and absence of 0.25% PVP or 0.20% HMPC were equilibrated for 3 days in the donor chamber of Franz diffusion cells holding hairless mouse skin.…”

Section: Dermal Rectal and Pulmonary Applications Of Cyclodextrinsmentioning

confidence: 99%

Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug Delivery

Rajewski¹,

Stella²

1996

Journal of Pharmaceutical Sciences

763

374

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The objective of this Review is to summarize and critique recent findings and applications of both unmodified and modified cyclodextrins for in vivo drug delivery. This review focuses on the use of cyclodextrins for parenteral, oral, ophthalmic, and nasal drug delivery. Other routes including dermal, rectal, and pulmonary delivery are also briefly addressed. This Review primarily focuses on newer findings concerning cyclodextrin derivatives which are likely to receive regulatory acceptance due to improved aqueous solubility and safety profiles as compared to the unmodified cyclodextrins. Many of the applications reviewed involve the use of hydroxypropyl-beta-cyclodextrins (HP-beta-CDs) and sulfobutylether-beta-cyclodextrins (SBE-beta-CDs) which show promise of greater safety while maintaining the ability to form inclusion complexes. The advantages and limitations of HP-beta-CD, SBE-beta-CD, and other cyclodextrins are addressed.

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“…The different chemically modified cyclodextrins like hydroxylpropyl β-cyclodextrin and dimethyl β-cyclodextrin used as penetration enhancers which act by solubilizing lipophilic drugs and constantly supplying the dissolved drug molecules to the skin surface where they partition into the skin barrier[5]. The cyclodextrins also alleviate the drug induced primary irritation of skin by complexation[6]. Urea is a physiological component of NMF (natural moisturizing factor) of the skin, has mild keratolytic effect and hence is used in the topical drug formulations.…”

mentioning

confidence: 99%

Effect of different carriers on in vitro permeation of meloxicam through rat skin

Saleem¹,

Bala²,

Liyakat³

et al. 2010

Indian J Pharm Sci

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The ability of β-cyclodextrin, hydroxypropyl-β-cyclodextrin, polyvinyl pyrrolidone and urea to influence the percutaneous absorption of meloxicam through isolated rat skin was evaluated. Carrier complex were prepared by kneading method in 1:1 and 1:2 in molar ratios for β-cyclodextrin and hydroxypropyl-β-cyclodextrin and in 1:1, 1:3 and 1:5 in weight ratios for polyvinyl pyrrolidone and urea. The complexes were characterized by IR, DSC and evaluated for solubility, dissolution and skin permeability. The solubility, dissolution and permeability of meloxicam were enhanced by using the carriers. The influence of cyclodextrins, polyvinyl pyrrolidone and urea on in vitro permeation of meloxicam through rat skin was investigated by incorporation of prepared carrier complex in 1% carbopol gel. The prepared gel was evaluated for drug content, pH and viscosity and in vitro permeation. All the percutaneous parameters like flux (Jss), amount permeated (Q6), diffusivity (D), permeability coefficient (Kp), partition coefficient (K) and release rate constant (k) were calculated statistically. In vitro permeation study showed the trend that the penetration flux and enhancement factor increases with increasing concentration of β-cyclodextrin and hydroxypropyl-β-cyclodextrin and then decrease dramatically in case of hydroxypropyl-β-cyclodextrin gel formulation with the increase to 1:2 ratio. Similar changes in pattern of permeation were also observed with polyvinyl pyrrolidone and urea carrier complex. These findings concluded that the carriers cyclodextrins, polyvinyl pyrrolidone and urea could be used as transdermal permeation enhancer in topical preparation of meloxicam.

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Alleviation of prochlorperazine-induced primary irritation of skin by cyclodextrin complexation.

Cited by 36 publications

References 0 publications

Design and Evaluation of Cyclodextrin-Based Drug Formulation

Design and Evaluation of Cyclodextrin-Based Drug Formulation

Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug Delivery

Effect of different carriers on in vitro permeation of meloxicam through rat skin

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