Development and optimization of in-situ gels for vaginal delivery of metronidazole and curcumin via box-behnken design: In vitro characterization and anti-trichomonas activity

POJARANİ, Leyla BEBA; Baloğlu, Esra; Süer, Kaya; Güler, Emrah; Burgaz, E. Vildan; Kunter, İmge

doi:10.1016/j.jddst.2023.104739

Cited by 6 publications

(1 citation statement)

References 65 publications

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“…The TEM micrographs showed that PX forms micelles that have the tendency to align along the BNC nanofibrils. PX micelles of around 10-20 nm were previously observed by TEM and DLS [75,115], and micelles with a mean diameter of 60 nm were evaluated for a poloxamer P403-heparin system [116]. The micelles in Figure 2d appear to have the same size as the diameter of some of the bacterial cellulose nanofibrils, which were evaluated in our previous study of BNC to be around 10-20 nm [26], or around 40-60 nm in another study [29], which could favor their interactions.…”

Section: Discussionmentioning

confidence: 79%

Bioactive-Loaded Hydrogels Based on Bacterial Nanocellulose, Chitosan, and Poloxamer for Rebalancing Vaginal Microbiota

Moraru,

Dima,

Tritean

et al. 2023

Pharmaceuticals

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Biocompatible drug-delivery systems for soft tissue applications are of high interest for the medical and pharmaceutical fields. The subject of this research is the development of hydrogels loaded with bioactive compounds (inulin, thyme essential oil, hydro-glycero-alcoholic extract of Vitis vinifera, Opuntia ficus-indica powder, lactic acid, citric acid) in order to support the vaginal microbiota homeostasis. The nanofibrillar phyto-hydrogel systems developed using the biocompatible polymers chitosan (CS), never-dried bacterial nanocellulose (NDBNC), and Poloxamer 407 (PX) incorporated the water-soluble bioactive components in the NDBNC hydrophilic fraction and the hydrophobic components in the hydrophobic core of the PX fraction. Two NDBNC-PX hydrogels and one NDBNC-PX-CS hydrogel were structurally and physical-chemically characterized using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD), transmission electron microscopy (TEM), and rheology. The hydrogels were also evaluated in terms of thermo-responsive properties, mucoadhesion, biocompatibility, and prebiotic and antimicrobial effects. The mucin binding efficiency of hydrogel base systems was determined by the periodic acid/Schiff base (PAS) assay. Biocompatibility of hydrogel systems was determined by the MTT test using mouse fibroblasts. The prebiotic activity was determined using the probiotic strains Limosilactobacillus reuteri and Lactiplantibacillus plantarum subsp. plantarum. Antimicrobial activity was also assessed using relevant microbial strains, respectively, E. coli and C. albicans. TEM evidenced PX micelles of around 20 nm on NDBNC nanofibrils. The FTIR and XRD analyses revealed that the binary hydrogels are dominated by PX signals, and that the ternary hydrogel is dominated by CS, with additional particular fingerprints for the biocompounds and the hydrogel interaction with mucin. Rheology evidenced the gel transition temperatures of 18–22 °C for the binary hydrogels with thixotropic behavior and, respectively, no gel transition, with rheopectic behavior for the ternary hydrogel. The adhesion energies of the binary and ternary hydrogels were evaluated to be around 1.2 J/m2 and 9.1 J/m2, respectively. The hydrogels exhibited a high degree of biocompatibility, with the potential to support cell proliferation and also to promote the growth of lactobacilli. The hydrogel systems also presented significant antimicrobial and antibiofilm activity.

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Section: Discussionmentioning

confidence: 79%

Bioactive-Loaded Hydrogels Based on Bacterial Nanocellulose, Chitosan, and Poloxamer for Rebalancing Vaginal Microbiota

Moraru,

Dima,

Tritean

et al. 2023

Pharmaceuticals

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Hybrid Nanoparticles Dual‐Loaded With Curcumin and Benzydamine Hydrochloride for the Treatment of Vulvovaginal Candidiasis: From Development to Biological Application In Vitro and In Vivo

Carvalho,

Domingues,

Marena

et al. 2024

Advanced Therapeutics

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Vulvovaginal candidiasis represents a public health challenge due to its reports of high incidence and recurrence. These are caused by host‐related factors like compromised immune system, or pathogen‐related factors, such as resistance to antifungal agents, making this medical problem desirable to develop new therapeutic options. In this context, natural origin substances like curcumin, are increasingly treatment alternatives. However, some curcumin properties limit its therapeutic application, such as insolubility in aqueous solvents, which leads to low bioavailability. Nevertheless, nanotechnology association with drugs of plant origin proves to be a promising alternative to overcome the reported drawbacks. Despite being caused by a fungus, patients suffer significantly from the inflammation resulting from this disease, thus this study aimed to develop a hybrid carrier nanoformulation by microfluidics loaded with two drugs, benzydamine hydrochloride (an anti‐inflammatory drug) and curcumin (an antifungal drug). Transmission electron cryomicroscopy combined with energy dispersive X‐ray analysis confirmed that the nanoparticle is properly developed. Through in vitro biological studies, it is possible to observe that, in addition to being safe, the encapsulation of both drugs in the nanocarrier drastically reduced their cytotoxicity. Finally, although the final nanoformulation does not show in vitro activity, the in vivo study indicated therapeutic potential.

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In-situ gel: A smart carrier for drug delivery

Garg,

Agrawal,

Singh Chauhan

et al. 2024

International Journal of Pharmaceutics

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Development and optimization of in-situ gels for vaginal delivery of metronidazole and curcumin via box-behnken design: In vitro characterization and anti-trichomonas activity

Cited by 6 publications

References 65 publications

Bioactive-Loaded Hydrogels Based on Bacterial Nanocellulose, Chitosan, and Poloxamer for Rebalancing Vaginal Microbiota

Bioactive-Loaded Hydrogels Based on Bacterial Nanocellulose, Chitosan, and Poloxamer for Rebalancing Vaginal Microbiota

Hybrid Nanoparticles Dual‐Loaded With Curcumin and Benzydamine Hydrochloride for the Treatment of Vulvovaginal Candidiasis: From Development to Biological Application In Vitro and In Vivo

In-situ gel: A smart carrier for drug delivery

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