Validation of spectrophotometric method to quantify cabotegravir in simulated vaginal fluid and porcine vaginal tissue in ex vivo permeation and retention studies from thermosensitive and mucoadhesive gels

Sulistiawati,; Enggi, Cindy Kristina; Isa, Hansel Tridatmojo; Wijaya, Stevens; Ardika, Komang Agus Rai; Asri, Rangga Meidianto; Donnelly, Ryan F.; Permana, Andi Dian

doi:10.1016/j.saa.2021.120600

Cited by 20 publications

(2 citation statements)

References 24 publications

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“…Therefore, several authors have used this type of tissue in permeation studies for pharmacokinetic and tolerability assessments (Davis et al, 2003; Gómez‐Segura et al, 2020), as well as in the development of new formulations (Enggi et al, 2022). In the present study, it was not feasible to conduct a solubility assessment because the commercially available API is in the form of a dispersion in hydroxypropyl methylcellulose, as discussed in previous sections.…”

Section: Resultsmentioning

confidence: 99%

Development and validation of a stability‐indicating method, structural elucidation of new degradation products from misoprostol by LC–MS time‐of‐flight, and an ex vivo study of vaginal permeation

da Silva,

Duarte,

Ribeiro

et al. 2024

Biomedical Chromatography

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Misoprostol (MSP) is commonly prescribed in obstetrics and gynecology clinical practice for labor induction, cervical ripening, first‐trimester pregnancy termination, and the treatment of postpartum hemorrhage. Furthermore, there is a lack of comprehensive discussion evaluating how different commercially available formulations influence the overall efficacy of MSP, even though reports indicate issues with the quality of these formulations, particularly regarding stability and vaginal absorption processes. This study investigates the stability of MSP under acidic conditions and its in vitro permeation using swine vaginal mucosa. A forced degradation study was conducted using 0.2 M HCl, and a high‐efficiency LC method was developed. Three degradation products were identified and characterized using electrospray ionization–high‐resolution quadrupole‐time‐of‐flight–MS, with respective m/z values of 391.2508, 405.2705, and 387.2259, respectively. These results suggest that the degradation mechanism involves dehydration of the β‐hydroxy ketone moiety, followed by isomerization to its most resonance‐stable form and de‐esterification. Finally, the in vitro permeation study revealed that the esterified form of MSP was unable to permeate the mucosa and required prior degradation for any component to be detected in the receptor fluid.

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Section: Resultsmentioning

confidence: 99%

Development and validation of a stability‐indicating method, structural elucidation of new degradation products from misoprostol by LC–MS time‐of‐flight, and an ex vivo study of vaginal permeation

da Silva,

Duarte,

Ribeiro

et al. 2024

Biomedical Chromatography

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show abstract

“…Unfortunately, the high water content of conventional gel caused it to be easily rinsed away by vaginal physiological fluid during application. In situ thermoresponsive gel is created employing thermogelling polymers, which enable the conversion of a free-flowing fluid into a solid gel at physiological temperature, to solve this issue [ 16 , 17 , 18 , 19 , 20 ]. As a result, this study proposes in situ vaginal gel to give prolonged contact with the mucosal lining of vagina, increasing medication absorption and therapeutic effectiveness.…”

Section: Introductionmentioning

confidence: 99%

Development of Thermoresponsive Hydrogels with Mucoadhesion Properties Loaded with Metronidazole Gel-Flakes for Improved Bacterial Vaginosis Treatment

et al. 2023

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Bacterial vaginosis is an infectious disease that has significantly affected women’s health. Metronidazole has been widely used as a drug for treating bacterial vaginosis. Nevertheless, the currently available therapies have been found to be inefficient and inconvenient. Here, we developed the combination approach of gel flake and thermoresponsive hydrogel systems. The gel flakes were prepared using gellan gum and chitosan, showing that the incorporation of metronidazole was able to provide a sustained release pattern for 24 h with an entrapment efficiency of >90%. Moreover, the gel flakes were incorporated into Pluronics-based thermoresponsive hydrogel using the combination of Pluronic F127 and F68. The hydrogels were found to exhibit the desired thermoresponsive properties, showing sol-gel transition at vaginal temperature. Following the addition of sodium alginate as a mucoadhesive agent, the hydrogel was retained in the vaginal tissue for more than 8 h, with more than 5 mg of metronidazole retained in the ex vivo evaluation. Finally, using the bacterial vaginosis infection model in rats, this approach could decrease the viability of Escherichia coli and Staphylococcus aureus with reduction percentages of more than 95% after 3 days of treatment, with the healing ability similar to normal vaginal tissue. In conclusion, this study offers an effective approach for the treatment of bacterial vaginosis.

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Development of a Cr2AlC MAX phase/g-C3N4 composite-based electrochemical sensor for accurate cabotegravir determination in pharmaceutical and biological samples

Bouali,

Genc,

Erk

et al. 2024

Microchim Acta

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Validation of spectrophotometric method to quantify cabotegravir in simulated vaginal fluid and porcine vaginal tissue in ex vivo permeation and retention studies from thermosensitive and mucoadhesive gels

Cited by 20 publications

References 24 publications

Development and validation of a stability‐indicating method, structural elucidation of new degradation products from misoprostol by LC–MS time‐of‐flight, and an ex vivo study of vaginal permeation

Development and validation of a stability‐indicating method, structural elucidation of new degradation products from misoprostol by LC–MS time‐of‐flight, and an ex vivo study of vaginal permeation

Development of Thermoresponsive Hydrogels with Mucoadhesion Properties Loaded with Metronidazole Gel-Flakes for Improved Bacterial Vaginosis Treatment

Development of a Cr2AlC MAX phase/g-C3N4 composite-based electrochemical sensor for accurate cabotegravir determination in pharmaceutical and biological samples

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