Synthesis and Characterization of Chitosan-Decorated Nanoemulsion Gel of 5-Fluorouracil for Topical Delivery

Nawaz, Asif; Latif, Muhammad Shahid; Alnuwaiser, Maha Abdallah; Ullah, Shafi; Iqbal, Muhammad; Alfatama, Mulham; Lim, Vuanghao

doi:10.3390/gels8070412

Cited by 19 publications

(11 citation statements)

References 34 publications

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“…On the other hand, it is sensitive to pH, which is not suitable for oral. According to the literature [ 13 , 21 ], GO/HPC/CS@5-Fu aerogel is suitable for skin implants or intratumoral injection. Future work will focus on skin drug retention and tumor growth inhibition testing after drug administration.…”

Section: Resultsmentioning

confidence: 99%

“…Among the natural polysaccharides, chitosan (CS) has attracted much attention in medical fields [ 11 , 12 ] and is widely used for the loading and release of 5-Fu. CS-decorated nanoemulsion gel used for the topical delivery of 5-Fu was reported by the group of Lim [ 13 ]. The incorporation of a nanoemulsion into CS gel extended the half-life and enhanced the skin’s drug retention, which is suitable for the treatment of melanoma.…”

Section: Introductionmentioning

confidence: 99%

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Fabrication and Evaluation of Graphene Oxide/Hydroxypropyl Cellulose/Chitosan Hybrid Aerogel for 5-Fluorouracil Release

Sang

Miao

Chen

et al. 2022

Gels

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The incorporation of graphene oxide (GO) into a polymeric drug carrier can not only enhance the loading efficiency but also reduce the initial burst and consequently improve the controllability of drug release. Firstly, 5-fluorouracil (5-Fu)-loaded hydroxypropyl cellulose/chitosan (HPC/CS@5-Fu) and GO/HPC/CS@5-Fu aerogels were successfully fabricated through chemical cross-linking with glutaraldehyde. Then, the obtained aerogels were characterized using scanning electron microscopy (SEM), Fourier transform infrared (FITR), X-ray diffraction (XRD), differential scanning calorimetry (DSC), thermogravimetry (TG), and the effect of HPC and GO content on the drug loading (DL) and encapsulation efficiency (EE) for the two aerogels were investigated, respectively. Finally, the drug release behavior of the GO/HPC/CS@5-Fu aerogels with different GO content was evaluated at two different pH values, and four kinds of kinetic models were used to evaluate the release behavior.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Fabrication and Evaluation of Graphene Oxide/Hydroxypropyl Cellulose/Chitosan Hybrid Aerogel for 5-Fluorouracil Release

Sang

Miao

Chen

et al. 2022

Gels

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“…The ATR-FTIR spectra of drug 5FU, alginate, chitosan, nanoparticles, and hydrogels are shown in Figure 2 . We found that 5FU has the characteristic peaks at 2992 (N–H stretching vibrations), 2883 (C=H stretching vibrations), 1723 (C=O group of ketone), 1505 and 1253 cm −1 (stretching vibration of C=N and C=F, respectively) [ 38 ]. The characteristic FTIR peaks of chitosan were at 3390, 2977, 1665, and 1401 cm −1 , and for alginate were at 3121, 2928, 1404, and 1050 cm −1 .…”

Section: Resultsmentioning

confidence: 99%

“…The temperature of the medium was maintained at 32 and 37 °C. At specific time intervals (0, 0.5, 1, 2, 4, 8, 12, 16, 20, and 24 h), 2 mL of sample was collected and analyzed on UV spectroscopy at 265 nm [ 38 ]. The in vitro release data obtained, were fitted into Korsmeyer-Peppas equation (Equation (3)) for investigation of drug release mechanism.…”

Section: Methodsmentioning

confidence: 99%

Formulation and Evaluation of Chitosan-Gelatin Thermosensitive Hydrogels Containing 5FU-Alginate Nanoparticles for Skin Delivery

Nawaz

Ullah

Alnuwaiser

et al. 2022

Gels

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(1) Background: Chitosan-gelatin-based thermosensitive hydrogel containing 5FU-alginate nanoparticles was formulated for the effective and sustained delivery of 5FU to the skin. (2) Methods: Alginate, a polysaccharide was used for the formulation of nanoparticles using a spray drying technique. Size, zeta potential, and surface morphology were investigated using a zetasizer and scanning electron microscope. The hydrogel was fabricated using chitosan and gelatin. Several important analyses were used to characterize these prepared topical hydrogels. The pH, visual transparency, rheological behavior, and swelling index of the prepared hydrogels were evaluated. The in vitro release studies were performed at different pH (5.5 and 7.4) and temperature (32 and 37 °C) conditions using a Franz diffusion cell. Ex vivo permeation and in vivo studies were performed using Sprague Dawley rats. (3) Results: Results show that spherical nanoparticles were produced at sizes of 202–254 nm and with zeta potentials of −43 to −38 mV. The prepared nanoparticles were successfully incorporated into chitosan-gelatin-based hydrogels using a glycerol 2-phosphate disodium salt hydrates crosslinker. Drug polymers and excipients compatibility and formulation of hydrogels was confirmed by ATR-FTIR results. The pH of the prepared hydrogels was in accordance with the skin pH. The viscosity of prepared hydrogel increased with temperature increase and phase transition (sol-gel transition) occurred at 34 °C. The release of drug was sustained in case of nanoparticles incorporated hydrogels (5FU-Alg-Np-HG) as compared to nanoparticles (5FU-Alg-Np) and simple hydrogels (5FU-HG) (ANOVA; p < 0.05). The premature and initial burst release of 5FU was prevented using 5FU-Alg-Np-HG. The release mechanism of 5FU from the 5FU-Alg-Np-HG diffusion was followed by swelling and erosion, as suggested by Korsmeyer-Peppas model. The prepared hydrogel proved to be non-irritant. Ex vivo permeation study across rat’s skin suggests that permeability of nanoparticles (5FU-Alg-Np) was higher than the 5FU-Alg-Np-HG (ANOVA; p < 0.05). However, skin-related drug retention of 5FU-Alg-Np-HG was significantly higher than the 5FU solution, 5FU-Alg-Np, and 5FU-HG (ANOVA; p < 0.05). This was due to swelling of hydrogels in the lower layers of skin where the temperature is 37 °C. The higher concentration of 5FU in the skin is helpful for treatment of local skin cancer, such as melanoma, and actinic keratosis. In vivo results also confirmed maximum AUC, t1/2, and skin-related drug retention of 5FU-Alg-Np-HG. (4) Conclusion: Chitosan-gelatin-based hydrogels containing 5FU-Alg-Np possess exceptional properties, and can be used for the sustained delivery of 5FU for the treatment of local skin cancers.

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“…It is the thermostability that differentiates nanoemulsions from conventional emulsions, which have good kinetic stability but eventually phase separate with time. Thermodynamic stability studies ensure the stability of the optimized formulation [ 60 , 61 , 62 ]. The metastable formation can be detected by these tests.…”

Section: Resultsmentioning

confidence: 99%

Thermosensitive Hydrogels Loaded with Resveratrol Nanoemulsion: Formulation Optimization by Central Composite Design and Evaluation in MCF-7 Human Breast Cancer Cell Lines

Aldawsari

Badr-Eldin

Nair

et al. 2022

Gels

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The second most common cause of mortality among women is breast cancer. A variety of natural compounds have been demonstrated to be beneficial in the management of various malignancies. Resveratrol is a promising anticancer polyphenolic compound found in grapes, berries, etc. Nevertheless, its low solubility, and hence its low bioavailability, restrict its therapeutic potential. Therefore, in our study, we developed a thermosensitive hydrogel formulation loaded with resveratrol nanoemulsion to enhance its bioavailability. Initially, resveratrol nanoemulsions were formulated and optimized utilizing a central composite-face-centered design. The independent variables for optimization were surfactant level, homogenization speed, and time, while the size and zeta potential were the dependent variables. The optimized nanoemulsion formulation was converted into a sensitive hydrogel using poloxamer 407. Rheological studies proved the formation of gel consistency at physiological temperature. Drug loading efficiency and in vitro drug release from gels were also analyzed. The drug release mechanisms from the gels were assessed using various mathematical models. The effect of the optimized thermosensitive resveratrol nanoemulsion hydrogel on the viability of human breast cancer cells was tested using MCF-7 cancer cell lines. The globule size of the selected formulation was 111.54 ± 4.16 nm, with a zeta potential of 40.96 ± 3.1 mV. Within 6 h, the in vitro release profile demonstrated a release rate of 80%. According to cell line studies, the produced hydrogel of resveratrol nanoemulsion was cytotoxic to breast cancer cells. Overall, the results proved the developed nanoemulsion-loaded thermosensitive hydrogel is a promising platform for the effective delivery of resveratrol for the management of breast cancer.

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Synthesis and Characterization of Chitosan-Decorated Nanoemulsion Gel of 5-Fluorouracil for Topical Delivery

Cited by 19 publications

References 34 publications

Fabrication and Evaluation of Graphene Oxide/Hydroxypropyl Cellulose/Chitosan Hybrid Aerogel for 5-Fluorouracil Release

Fabrication and Evaluation of Graphene Oxide/Hydroxypropyl Cellulose/Chitosan Hybrid Aerogel for 5-Fluorouracil Release

Formulation and Evaluation of Chitosan-Gelatin Thermosensitive Hydrogels Containing 5FU-Alginate Nanoparticles for Skin Delivery

Thermosensitive Hydrogels Loaded with Resveratrol Nanoemulsion: Formulation Optimization by Central Composite Design and Evaluation in MCF-7 Human Breast Cancer Cell Lines

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