The effect of permeation enhancers on the viscosity and the release profile of transdermal hydroxypropyl methylcellulose gel formulations containing diltiazem HCl

Karakatsani, Marianthi; Dedhiya, Mahendra G.; Plakogiannis, Fotios M.

doi:10.3109/03639041003695105

Cited by 26 publications

(15 citation statements)

References 22 publications

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“…However, the permeation enhancement effect reached maximum at a certain viscosity and then remained rather constant despite further increases in the viscosity. This is not in agreement with some of the findings reported, where the increased viscosity of drug solution was found to decrease drug permeation and prolong drug release [34]. The anti‐aggregation and plasticizer properties of PVP could also possibly enhance Ce6 molecules transport across the CAM.…”

Section: Discussioncontrasting

confidence: 86%

Ex-vivo permeation study of chlorin e6-polyvinylpyrrolidone complexes through the chick chorioallantoic membrane model

Chutoprapat

Chan

Heng

2014

Journal of Pharmacy and Pharmacology

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Section: Discussioncontrasting

confidence: 86%

Ex-vivo permeation study of chlorin e6-polyvinylpyrrolidone complexes through the chick chorioallantoic membrane model

Chutoprapat

Chan

Heng

2014

Journal of Pharmacy and Pharmacology

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“…The visual aspect of this batch, It can clearly be seen how the viscosity drops sharply to below 100 mPa•s when a surfactant is added. This effect, which is attributed to the decrease in tension between polymer chains, has been observed for these same surfactants and for many others [33][34][35]. In these batches, the micelles in the surfactants act as a spatial impediment and prevent the free organization of the HPMC polymer chains and their subsequent gelation.…”

Section: Penetration and Detachment Worksupporting

confidence: 59%

Mucoadhesive Vaginal Discs based on Cyclodextrin and Surfactants for the Controlled Release of Antiretroviral Drugs to Prevent the Sexual Transmission of HIV

et al. 2020

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The strategies for developing vaginal microbicides to protect women against human immunodeficiency virus (HIV) sexual transmission are constantly changing. Although the initial dosage forms required daily administration to offer effective protection, the trend then moved towards sustained-release dosage forms that require less frequency of administration in order to improve women’s compliance with the treatment. Nevertheless, another possible strategy is to design on-demand products that can be used in a coitally-dependent manner and only need to be administered immediately before intercourse to offer protection. Vaginal discs based on freeze-dried hydroxypropylmethyl cellulose gels have been developed for this purpose, containing two surfactants, i.e., sodium dodecyl sulphate and polysorbate 60, alone or in combination with 2-hydroxypropyl-β-cyclodextrin, to achieve a formulation capable of incorporating both hydrophilic and lipophilic drugs. Several studies have been carried out to evaluate how the inclusion of these substances modifies the structure of gels (viscosity and consistency studies) and the porosimetry of the freeze-dried discs (scanning electron microscopy micrographs, mechanical properties, swelling behaviour). The drug release and mucoadhesive properties of the discs have also been evaluated with a view to their clinical application. The systems combining sodium dodecyl sulphate and 2-hydroxypropyl-β-cyclodextrin were found to be adequate for the vaginal administration of both Tenofovir and Dapivirine and also offer excellent mucoadhesion to vaginal tissue; these discs could therefore be an interesting option for a coitally-dependent administration to protect women against HIV transmission.

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“…The partition coefficient values of drugs in n-octanol/water were determined 20,21 . Then, 20 mL of n-octanol (saturated with water) was added to an equivalent volume of coarse drugs saturated solution in water (saturated with n-octanol) in a separating funnel.…”

Section: Determination Of Log Pmentioning

confidence: 99%

Influence of drug physicochemical characteristics onin vitrotransdermal absorption of hydrophobic drug nanosuspensions

Shen¹,

Li²,

Shen³

et al. 2015

Drug Development and Industrial Pharmacy

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The purpose of this paper was to study the influence of drug physicochemical characteristics on in vitro transdermal absorption of hydrophobic drug nanosuspensions. Four drug nanosuspensions were produced by high-pressure homogenization technique, which were the same in stabilizer and similar in particle size. Differential scanning calorimetry and powder X-ray diffraction analysis showed that the crystalline state of the nanocrystals did not change. In vitro permeation study demonstrated that the drug nanosuspensions have a higher rate of permeation that ranged from 1.69- to 3.74-fold compared to drug microsuspensions. Correlation analysis between drug physicochemical properties and Jss revealed that log P and pKa were factors that influenced the in vitro transdermal absorption of hydrophobic drug nanosuspensions, and drugs with a log P value around 3 and a higher pKa value (when pKa < pH+2) would gain higher Jss in this paper.

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The effect of permeation enhancers on the viscosity and the release profile of transdermal hydroxypropyl methylcellulose gel formulations containing diltiazem HCl

Abstract: These findings indicate that to formulate DTM HCl into a hydroxypropyl methylcellulose gel the enhancers of choice should be polysorbate 80, myristic acid, DMSO, NMP, and IPM or combinations thereof.

Cited by 26 publications

References 22 publications

Ex-vivo permeation study of chlorin e6-polyvinylpyrrolidone complexes through the chick chorioallantoic membrane model

Ex-vivo permeation study of chlorin e6-polyvinylpyrrolidone complexes through the chick chorioallantoic membrane model

Mucoadhesive Vaginal Discs based on Cyclodextrin and Surfactants for the Controlled Release of Antiretroviral Drugs to Prevent the Sexual Transmission of HIV

Influence of drug physicochemical characteristics onin vitrotransdermal absorption of hydrophobic drug nanosuspensions

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