Bioadhesive emulsions for control release of progesterone resistant to vaginal fluids clearance

Campaña-Seoane, Maria; Peleteiro, Aaron; Laguna, Reyes; Otero-Espinar, Francisco J.

doi:10.1016/j.ijpharm.2014.10.066

Cited by 37 publications

(21 citation statements)

References 38 publications

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“…Because the volume of vaginal fluids usually varies from 0.5 to 0.75 mL20, 21, the formulations were mixed with SVF to simulate extreme dilution in the in vivo circumstance. As shown in Fig.…”

Section: Resultsmentioning

confidence: 99%

In vivo retention of poloxamer-based in situ hydrogels for vaginal application in mouse and rat models

Liu

Yang

Feng

et al. 2017

Acta Pharmaceutica Sinica B

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The purpose of this study is to evaluate the in vivo retention capabilities of poloxamer-based in situ hydrogels for vaginal application with nonoxinol-9 as the model drug. Two in situ hydrogel formulations, which contained 18% poloxamer 407 plus 1% poloxamer 188 (GEL1, relative hydrophobic) or 6% poloxamer 188 (GEL2, relative hydrophilic), were compared with respect to the rheological properties, in vitro hydrogel erosion and drug release. The vaginal retention capabilities of these hydrogel formulations were further determined in two small animal models, including drug quantitation of vaginal rinsing fluid in mice and isotope tracing with 99mTc in rats. The two formulations exhibited similar phase transition temperatures ranging from 27 to 32 °C. Increasing the content of poloxamer 188 resulted in higher rheological moduli under body temperature, but slightly accelerated hydrogel erosion and drug release. When compared in vivo, GEL1 was eliminated significantly slower in rat vagina than GEL2, while the vaginal retention of these two hydrogel formulations behaved similarly in mice. In conclusion, increases in the hydrophilic content of formulations led to faster hydrogel erosion, drug release and intravaginal elimination. Rats appear to be a better animal model than mice to evaluate the in situ hydrogel for vaginal application.

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Section: Resultsmentioning

confidence: 99%

In vivo retention of poloxamer-based in situ hydrogels for vaginal application in mouse and rat models

Liu

Yang

Feng

et al. 2017

Acta Pharmaceutica Sinica B

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“…The extensibility of PGZ-NE was examined in triplicate following the previously described method [22]. A sample of 0.15 g was placed on the center of the base plate of an extensometer followed by immediate placement of a glass plate (26.86 g) on top of the sample.…”

Section: Characterization Of Pgz-nementioning

confidence: 99%

Topical Pioglitazone Nanoformulation for the Treatment of Atopic Dermatitis: Design, Characterization and Efficacy in Hairless Mouse Model

et al. 2020

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Pioglitazone (PGZ) is a drug used to treat type 2 diabetes mellitus that has been reported to show additional therapeutic activities on diverse inflammatory parameters. The aim of this study was to optimize a topical PGZ-loaded nanoemulsion (PGZ-NE) in order to evaluate its effectiveness for treating atopic dermatitis (AD). The composition of the nanoformulation was established by pseudo-ternary diagram. Parameters such as physical properties, stability, in vitro release profile, and ex vivo permeation were determined. The efficacy study was carried out using oxazolone-induced AD model in hairless mice. PGZ-NE released the drug following a hyperbolic kinetic. Additionally, its properties provided high retention potential of drug inside the skin. Therapeutic benefits of PGZ-NE were confirmed on diverse events of the inflammatory process, such as reduction of lesions, enhancement of skin barrier function, diminished infiltration of inflammatory cells, and expression of pro-inflammatory cytokines. These results were reinforced by atomic force microscope (AFM), which demonstrated the ability of the formulation to revert the rigidification caused by oxazolone and consequently improve the elasticity of the skin. These results suggest that PGZ-NE may be a promising treatment for inflammatory dermatological conditions such as AD.

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“…Mucoadhesion strength was evaluated in triplicate using a TA.XT Plus Texture analyzer (Stable Micro Systems Products, Godalming, UK) following methods previously described by Akhter et al [42] and Campaña-Seoane et al [43] with some modifications. Bovine corneas were placed beneath double-sided tape at the end of the probe.…”

Section: In Vitro Mucoadhesive Studiesmentioning

confidence: 99%

“…Several in vitro techniques have been reported to study mucoadhesion [55]. The in vitro tensile test is widely used to assess mucoadhesive strength in terms of the detachment force needed to separate two surfaces [43,56]. The mucoadhesion strength of the formulations is summarized in Table 5.…”

Section: Mucoadhesion Studiesmentioning

confidence: 99%

In Vitro and Ex Vivo Evaluation of Nepafenac-Based Cyclodextrin Microparticles for Treatment of Eye Inflammation

et al. 2020

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The aim of this study was to design and evaluate novel cyclodextrin (CD)-based aggregate formulations to efficiently deliver nepafenac topically to the eye structure, to treat inflammation and increase nepafenac levels in the posterior segment, thus attenuating the response of inflammatory mediators. The physicochemical properties of nine aggregate formulations containing nepafenac/γ-CD/hydroxypropyl-β (HPβ)-CD complexes as well as their rheological properties, mucoadhesion, ocular irritancy, corneal and scleral permeability, and anti-inflammatory activity were investigated in detail. The results were compared with a commercially available nepafenac suspension, Nevanac® 3 mg/mL. All formulations showed microparticles, neutral pH, and negative zeta potential (–6 to –27 mV). They were non-irritating and nontoxic and showed high permeation through bovine sclera. Formulations containing carboxymethyl cellulose (CMC) showed greater anti-inflammatory activity, even higher than the commercial formulation, Nevanac® 0.3%. The optimized formulations represent an opportunity for topical instillation of drugs to the posterior segment of the eye.

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Bioadhesive emulsions for control release of progesterone resistant to vaginal fluids clearance

Cited by 37 publications

References 38 publications

In vivo retention of poloxamer-based in situ hydrogels for vaginal application in mouse and rat models

In vivo retention of poloxamer-based in situ hydrogels for vaginal application in mouse and rat models

Topical Pioglitazone Nanoformulation for the Treatment of Atopic Dermatitis: Design, Characterization and Efficacy in Hairless Mouse Model

In Vitro and Ex Vivo Evaluation of Nepafenac-Based Cyclodextrin Microparticles for Treatment of Eye Inflammation

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