Towards a better understanding of thermally treated polycarbophil matrix tablets for controlled release

Baldassari, Sara; Cirrincione, Paola; Ailuno, Giorgia; Drava, Giuliana; Arpicco, Silvia Maria; Caviglioli, Gabriele

doi:10.1016/j.ijpx.2021.100098

Cited by 2 publications

(1 citation statement)

References 42 publications

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“…Polycarbophil showed a broad endothermic peak around 78.5 °C representing the evaporation of the free water present in pectin due to hydrophilic groups. Near to 130 °C, a slight shift and change in heat capacity termed as a "z event" was observed, indicating glass transition, and from 200 °C onwards the spectrum showed polymer degradation [34]. The interaction between two polymers in a PEC can be often described by DSC.…”

Section: Dscmentioning

confidence: 99%

Polyelectrolyte-Complex-Based Hydrogel Inserts for Vaginal Delivery of Posaconazole and Probiotics

Deshkar,

Yeole,

Mahore

et al. 2023

Gels

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Worldwide, 40 to 50% of women suffer from reproductive tract infections. Most of these infections are mixed infections, are recurrent and difficult to treat with antimicrobials or antifungals alone. For symptomatic relief of infections, oral antimicrobial therapy must be combined with topical therapy. The purpose of this work is to optimize and develop a polyelectrolyte complex (PEC) of chitosan/anion for the formulation of posaconazole- and probiotic-loaded vaginal hydrogel inserts with prolonged release and significant mucoadhesion. PECs were prepared using chitosan as cationic and carrageenan, pectin and polycarbophil as anionic polymers via a lyophilization technique. PEC formation was confirmed by scanning electron microscopy, Fourier transform infrared spectroscopy and differential scanning calorimetry, by observing changes in its surface, physical and thermal properties. The probiotic, Lactobacillus casei, was added to the PEC during the lyophilization process and the effect on the probiotic viability was studied. The PECs were further compressed along with posaconazole to form hydrogel inserts and optimized using a 32 full-factorial design. The hydrogel inserts were assessed for swelling behavior, drug release, in vitro mucoadhesion and in vitro antifungal activity. The chitosan–pectin hydrogel insert demonstrated excellent mucoadhesion (1.25 N), sustained drug release (88.2 ± 2.4% in 8 h) and a swelling index of 154.7%. The efficacy of hydrogel inserts was evaluated using in vitro study with a co-culture of Lactobacillus casei and Candida albicans. This study revealed an increase in Lactobacilli casei count and a significant drop in the viable count of Candida albicans (4-log reduction in 24 h), indicating the effectiveness of hydrogel inserts in alleviating the fungal infection. Overall, our study demonstrated the potential of the hydrogel insert for preventing vaginal infection and restoring normal vaginal microbiota.

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Section: Dscmentioning

confidence: 99%

Polyelectrolyte-Complex-Based Hydrogel Inserts for Vaginal Delivery of Posaconazole and Probiotics

Deshkar,

Yeole,

Mahore

et al. 2023

Gels

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Silicone matrices for controlled dexamethasone release: toward a better understanding of the underlying mass transport mechanisms

Rongthong

Qnouch

Gehrke

et al. 2023

Regenerative Biomaterials

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Dexamethasone-loaded silicone matrices offer an interesting potential as innovative drug delivery systems, e.g. for the treatment of inner ear diseases or for pacemakers. Generally, very long drug release periods are targeted: several years/decades. This renders the development and optimization of novel drug products cumbersome: Experimental feedback on the impact of the device design is obtained very slowly. A better understanding of the underlying mass transport mechanisms can help facilitating research in this field. A variety of silicone films was prepared in this study, loaded with amorphous or crystalline dexamethasone. Different polymorphic drug forms were investigated, the film thickness was altered and the drug optionally partially/completely exchanged by much more water-soluble dexamethasone phosphate. Drug release studies in artificial perilymph, SEM, optical microscopy, DSC, X-ray diffraction and Raman imaging were used to elucidate the physical states of the drugs & polymer, and of the systems’ structure as well as dynamic changes thereof upon exposure to the release medium. Dexamethasone particles were initially homogeneously distributed throughout the systems. The hydrophobicity of the matrix former very much limits the amounts of water penetrating into the system, resulting in only partial drug dissolution. The mobile drug molecules diffuse out into the surrounding environment, due to concentration gradients. Interestingly, Raman imaging revealed that even very thin silicone layers (<20 µm) can effectively trap the drug for prolonged periods of time. The physical state of the drug (amorphous, crystalline) did not affect the resulting drug release kinetics to a noteworthy extent.

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Towards a better understanding of thermally treated polycarbophil matrix tablets for controlled release

Cited by 2 publications

References 42 publications

Polyelectrolyte-Complex-Based Hydrogel Inserts for Vaginal Delivery of Posaconazole and Probiotics

Polyelectrolyte-Complex-Based Hydrogel Inserts for Vaginal Delivery of Posaconazole and Probiotics

Silicone matrices for controlled dexamethasone release: toward a better understanding of the underlying mass transport mechanisms

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