Design and Development of an &amp;lt;i&amp;gt;in Vitro&amp;lt;/i&amp;gt; Assay for Evaluation of Solid Vaginal Dosage Forms

Gupta, Jyoti; Tao, Jason Qihai; Garg, Sanjay; Al‐Kassas, Raida

doi:10.4236/pp.2011.24037

Cited by 11 publications

(7 citation statements)

References 13 publications

(17 reference statements)

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“…The dissolution test was carried out with using the enhancer cell equipped with Cuprophan membrane. This model reflects the conditions of the vaginal cavity more suitably as it enables maintaining microparticles in a reservoir where drug carriers slowly hydrate and form gel matrix from which drug is released [45]. As shown in Figure 4, all designed chitosan microparticles exhibited prolonged CLO release rates as compared to control—simple dispersion of CLO in the release medium.…”

Section: Resultsmentioning

confidence: 99%

Novel Spray Dried Glycerol 2-Phosphate Cross-Linked Chitosan Microparticulate Vaginal Delivery System—Development, Characterization and Cytotoxicity Studies

et al. 2016

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Chitosan microparticulate delivery systems containing clotrimazole were prepared by a spray drying technique using glycerol 2-phosphate as an ion cross-linker. The impact of a cross-linking ratio on microparticle characteristics was evaluated. Drug-free and drug-loaded unmodified or ion cross-linked chitosan microparticles were examined for the in vitro cytotoxicity in VK2/E6E7 human vaginal epithelial cells. The presence of glycerol 2-phosphate influenced drug loading and encapsulation efficacy in chitosan microparticles. By increasing the cross-linking ratio, the microparticles with lower diameter, moisture content and smoother surface were observed. Mucoadhesive studies displayed that all formulations possessed mucoadhesive properties. The in vitro release profile of clotrimazole was found to alter considerably by changing the glycerol 2-phosphate/chitosan ratio. Results from cytotoxicity studies showed occurrence of apoptotic cells in the presence of chitosan and ion cross-linked chitosan microparticles, followed by a loss of membrane potential suggesting that cell death might go through the mitochondrial apoptotic pathway.

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Section: Resultsmentioning

confidence: 99%

Novel Spray Dried Glycerol 2-Phosphate Cross-Linked Chitosan Microparticulate Vaginal Delivery System—Development, Characterization and Cytotoxicity Studies

et al. 2016

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“…The selection of a method for in vitro dissolution studies was a challenge given that dissolution of solid vaginal dosage forms has not been widely investigated. Some researchers recommend the use of dissolution testing methods used for suppositories (22).…”

Section: Drug Release Studies On the Polymeric Capletmentioning

confidence: 99%

Submicron Matrices Embedded in a Polymeric Caplet for Extended Intravaginal Delivery of Zidovudine

Mashingaidze

Choonara

Kumar

et al. 2017

AAPS J

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In this study, an intravaginal delivery system able to deliver an anti-HIV-1 agent for the purpose of potentially reducing HIV-1 transmission acting over an extended duration was successfully formulated. This delivery system was a composite polymeric caplet comprising zidovudine-loaded polyethylene glycol enclatherated pectin-mucin submicron matrices embedded within a poly (D,L-lactide), magnesium stearate, Kollidon® SR, and Carbopol® 974P NF-based polymeric caplet matrix. A three-factor and three-level Box-Behnken statistical design was utilized to optimize the polymeric caplet. The optimized directly compressed composite polymeric caplet hardness was 22.1 ± 0.3 N and the matrix resilience was 62.4 ± 0.6%. The swelling- and diffusion-controlled fractional zidovudine (AZT) release from the optimized caplet was 0.74 ± 0.01 in simulated vaginal fluid (SVF), which increased to 0.81 ± 0.21 in phosphate-buffered saline (PBS) simulating seminal fluid, over 30 days. Caplet matrix swelling was directly related to the percentage Carbopol 974P NF composition. An intravaginal system for AZT delivery was tested in the pig model over 28 days. X-ray analysis depicted delivery system swelling with matrix contrast fading over time as vaginal fluid permeated the matrix core. Plasma, vaginal fluid swab eluates, and tissue AZT concentrations were measured by gradient ultra-performance liquid chromatography (UPLC)-tandem photodiode array detection. Vaginal tissue and vaginal fluid swab eluate AZT concentrations remained above effective levels over 28 days and were higher than plasma AZT concentrations, availing a system with reduced systemic toxicity and more effective inhibition of viral replication at the site of entry.

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“…The theoretical amount of AZT was the proportional amount of AZT in the 100mg of SMMs in reference to the loading dose. AZT release from PEG-encl-PEC:MUC SMMs was performed using the dialysis membrane technique over 24 hours in a 100mL container filled with SVF (Gupta et al, 2011;Woolfson et al, 2010;Shaikh et al, 2009). The dissolution media (simulated vaginal fluid, SVF), was prepared according to Owen and Katz's as presented in Table 3 (Owen and Katz, 1999).…”

Section: Drug Encapsulation and Release From Smmsmentioning

confidence: 99%

“…Drug release was also performed in phosphate buffered saline (PBS pH 7.4) which acted as simulated semen (Gupta et al, 2011;Woolfson et al, 2010;Owen and Katz, 2005). The AZT-loaded SMMs and 2mLs SVF or PBS (similar medium as the bulk 100mL dissolution medium) were added into a dialysis tubing which had a molecular weight cut off of 12kDa…”

Section: Drug Encapsulation and Release From Smmsmentioning

confidence: 99%

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Poly(ethylene glycol) enclatherated pectin-mucin submicron matrices for intravaginal anti-HIV-1 drug delivery

Mashingaidze

Choonara

Kumar

et al. 2016

International Journal of Pharmaceutics

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Design and Development of an <i>in Vitro</i> Assay for Evaluation of Solid Vaginal Dosage Forms

Abstract: ABSTRACT

Cited by 11 publications

References 13 publications

Novel Spray Dried Glycerol 2-Phosphate Cross-Linked Chitosan Microparticulate Vaginal Delivery System—Development, Characterization and Cytotoxicity Studies

Novel Spray Dried Glycerol 2-Phosphate Cross-Linked Chitosan Microparticulate Vaginal Delivery System—Development, Characterization and Cytotoxicity Studies

Submicron Matrices Embedded in a Polymeric Caplet for Extended Intravaginal Delivery of Zidovudine

Poly(ethylene glycol) enclatherated pectin-mucin submicron matrices for intravaginal anti-HIV-1 drug delivery

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