Rheological evaluation of thermosensitive and mucoadhesive vaginal gels in physiological conditions

Chang, Jung Yun; Oh, Yu‐Kyoung; Choi, Han‐Gon; Kim, Yang Bae; Kim, Chong‐Kook

doi:10.1016/s0378-5173(02)00232-6

Cited by 192 publications

(118 citation statements)

References 39 publications

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“…It is evident from the results of the vaginal dilution studies that only SR-2P and the formulation with 15% w/w of Pluronic® F-127 and 1% w/w of Noveon® AA-1 resisted erosion under physiological diluted conditions of simulated fluids and shear (Table I). As per published literature, the physiological shear rates during the passive and coital stress ranges from 0.1 to 100 s −1 (19)(20)(21). Since SR-2P has resisted shear (50 rpm) and extreme dilution in simulated fluids, it was further characterized at the physiological simulated dilution and intermediate penile stress (70 rpm; Fig.…”

Section: Effect Of Shear Force On Placebo Gels Under Different Conditmentioning

confidence: 84%

“…In addition, an erosion assay was also used to measure the propensity for the gel to be washed off from the surface by vaginal fluid, semen, and mixture of simulants (19,20). It is evident from the results of the vaginal dilution studies that only SR-2P and the formulation with 15% w/w of Pluronic® F-127 and 1% w/w of Noveon® AA-1 resisted erosion under physiological diluted conditions of simulated fluids and shear (Table I).…”

Section: Effect Of Shear Force On Placebo Gels Under Different Conditmentioning

confidence: 99%

“…4). The entire biologically relevant range of shear rates (19)(20)(21) was applied to the whole placebo SR-2P gel in the present study (Figs. 4, 5, 6, and 7).…”

Section: Effect Of Shear Force On Placebo Gels Under Different Conditmentioning

confidence: 99%

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Formulation Development and Evaluation of Innovative Two-Polymer (SR-2P) Bioadhesive Vaginal Gel

2014

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The main objective of this investigation was to study the feasibility of developing a vaginal bioadhesive microbicide using a SRI's proprietary two-polymer gel platform (SR-2P). Several formulations were prepared with different combinations of temperature-sensitive polymer (Pluronic® F-127) and mucoadhesive polymer (Noveon® AA-1), producing gels of different characteristics. Prototype polymeric gels were evaluated for pH, osmolality, buffering capacity, and viscosity under simulated vaginal semen dilutions, and bioadhesivity using ex vivo mini pig vaginal tissues and texture analyzer. The pH of the polymeric gel formulations ranged from 5.1 to 6.4; the osmolality varied from 13 to 173 mOsm. Absolute viscosity ranged from 513 to 3,780 cPs, and was significantly reduced (1.5-to 3-fold) upon incubation with simulated vaginal and semen fluid mixture. Among the tested gels (indicated in the middle row as a molar ratio of a mixture of Noveon vs. Pluronic), only SR-2P retained gel structure upon dilution with simulated fluids and mild simulated coital stress. The pH of the SR-2P gel was maintained at about 4.6 in simulated vaginal fluid and also showed high peak force of adhesion in mini pig vaginal tissue. Furthermore, SR-2P gel caused no or only minimal irritation in a mouse vaginal irritation model. The results of this preliminary study demonstrated the potential application of SR-2P gel as a vaginal microbicide vehicle for delivery of anti-HIV agents.

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Section: Effect Of Shear Force On Placebo Gels Under Different Conditmentioning

confidence: 84%

Section: Effect Of Shear Force On Placebo Gels Under Different Conditmentioning

confidence: 99%

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Formulation Development and Evaluation of Innovative Two-Polymer (SR-2P) Bioadhesive Vaginal Gel

2014

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“…Including drugs (50,51) or various additives (54-56) have decreased T sol-gel of poloxamer formulations. These agents interfere in Poloxamer 407 micellization and alter the dehydration of hydrophobic PO blocks (29,57). Molecules like diclofenac, ethanol and HCl increase Tsol-gel while others (e.g., NaCl, Na 2 HPO 4 , NaH 2 PO 4 ) do the opposite (30,54).…”

Section: Discussionmentioning

confidence: 99%

Influence of Oleic Acid on the Rheology and in Vitro Release of Lumiracoxib from Poloxamer Gels

2010

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-Purpose. Transdermal delivery of anti-inflammatory lumiracoxib (LM) could be an interesting strategy to avoid the side effects associated with systemic delivery, but it is ineffective due to the drug poor skin penetration. We have investigated the effects of oleic acid (OA), a lipid penetration enhancer, on the in vitro release of LM from poloxamer-based delivery systems (PBDS). The rheological behavior (shear rate dependent viscosity) and gelation temperature through measurements of optimal sol-gel transition temperatures (T sol-gel ) were also carried out in these systems. Methods. In vitro release studies of LM from PBDS were performed using cellulose acetate as artificial membrane mounted in a diffusion system. The amount of LM released was divided by exposition area (µg/cm 2 ) and these values were plotted as function of the time (h). The flux of the drug across the membrane (J) was calculated from the slope of the linear portion of the plot and expressed as µg/cm 2 /h. The determination of viscosity was carried out at different shear rates (γ) between 0.1-1000 S -1 using a parallel plate rheometer. Oscillatory measurements using a cone-plate geometry rheometer surrounded by a double jacket with temperature varying 4-40°C, was used in order to determine T sol-gel . Results. Increase of both polymer and OA concentrations increases the viscosity of the gels and consequently reduces the in vitro LM release from the PBDS, mainly for gels containing OA at 10.0% (w/w) compared to other concentrations of the penetration enhancer. T sol-gel transition temperature was decreased by increasing viscosity; in some cases the formulation was already a gel at room temperature. Rheological studies showed a pseudoplastic behavior, which facilitates the flow and improves the spreading characteristics of the formulations. Conclusions. Taken together, the results showed that poloxamer gels are good potential delivery systems for LM, leading to a sustained release, and also have appropriate rheological characteristics.

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“…The mucoadhesive formulations, administered by rectal (Choi, Oh, and Kim 1998;Ryu et al 1999;Yahagi, Onishi, and Machida 1999), vaginal (Lee and Chien 1996;Valenta et al 2001;Ceschel et al 2001a;Cevher, Sahin, and Araman 2002;Chang et al 2002;Chien and Lee 2002;El-Kamel et al 2002;Maggi et al 2000), oral (Takeuchi et al 2003), buccal (Shojaei, Zhou, and Li 1998;Alur et al 1999;Han et al 1999;Choi and Kim 2000;Shin, Bum, and Choi 2000;Ceschel, Maffei, and Lombardi 2001b;Perioli et al 2004), nasal (Ugwoke et al 1999;Yahagi et al 2000;Pavelic, SkalkoBasnet, and Schubert, 2001;Hasçiçek, Gönül, and Erk 2003;58 E. CEVHER ET AL. Sales et al 2003), and ocular (Yun et al 1999;Ceulemans et al 2001) routes, have been prepared by using polymers showing appropriate adhesiveness.…”

Section: Human Papilloma Virus (Hpv) Causes Infection In the Genital mentioning

confidence: 99%

Evaluation of Mechanical and Mucoadhesive Properties of Clomiphene Citrate Gel Formulations Containing Carbomers and Their Thiolated Derivatives

Cevher

Taha²,

Orlu

et al. 2008

Drug Delivery

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Rheological evaluation of thermosensitive and mucoadhesive vaginal gels in physiological conditions

Cited by 192 publications

References 39 publications

Formulation Development and Evaluation of Innovative Two-Polymer (SR-2P) Bioadhesive Vaginal Gel

Formulation Development and Evaluation of Innovative Two-Polymer (SR-2P) Bioadhesive Vaginal Gel

Influence of Oleic Acid on the Rheology and in Vitro Release of Lumiracoxib from Poloxamer Gels

Evaluation of Mechanical and Mucoadhesive Properties of Clomiphene Citrate Gel Formulations Containing Carbomers and Their Thiolated Derivatives

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