Lyophilized sponges loaded with curcumin solid lipid nanoparticles for buccal delivery: Development and characterization

Hazzah, Heba A.; Farid, Ragwa M.; Nasra, Maha M A; El-Massik, Magda A.; Abdallah, Ossama Y.

doi:10.1016/j.ijpharm.2015.06.022

Cited by 76 publications

(42 citation statements)

References 28 publications

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“…However, the extremely poor aqueous-solubility and poor bioavailability of Cur have hampered its clinical uses for cancer treatment [11]. Therefore, nanoscale drug delivery systems including, liposomes [12] liquid crystal [13] solid lipid nanoparticles [14] nanoemulsion [15], and phospholipids complex [16], have been used as means to overcome these disadvantages. In particular, liposomes have been considered as a promising drug nanocarrier vehicle for Cur and many other chemotherapeutic drugs due to the potential to improve the bioavailability, pharmacokinetic and pharmacodynamics of these drugs.…”

Section: Introductionmentioning

confidence: 99%

Long-Circulating Curcumin-Loaded Liposome Formulations with High Incorporation Efficiency, Stability and Anticancer Activity towards Pancreatic Adenocarcinoma Cell Lines In Vitro

et al. 2016

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The incorporation of hydrophobic drugs into liposomes improve their bioavailability and leads to increased stability and anticancer activity, along with decreased drug toxicity. Curcumin (Cur) is a natural polyphenol compound with a potent anticancer activity in pancreatic adenocarcinoma (PA). In the present study, different types of Cur-loaded liposomal formulations were prepared and characterized in terms of size, shape, zeta potential, optimal drug-to-lipid ratio and stability at 4°C, 37°C; and in human plasma in vitro. The best formulation in terms of these parameters was PEGylated, cholesterol-free formulation based upon hydrogenated soya PC (HSPC:DSPE-PEG2000:Cur, termed H5), which had a 0.05/10 molar ratio of drug-to-lipid, was found to be stable and had a 96% Cur incorporation efficiency. All Cur-loaded liposomal formulations had potent anticancer activity on the PA cancer cell lines AsPC-1 and BxPC-3, and were less toxic to a normal cell line (NHDF). Furthermore, apoptosis-induction induced by Cur in PA cells was associated with morphological changes including cell shrinkage, cytoplasmic blebbing, irregularity in shape and the externalization of cell membrane phosphatidylserine, which was preceded by an increase in intracellular reactive oxygen species (ROS) generation and caspase 3/7 activation. Because the liposomal formulations tested here, especially the H5 variant which exhibited slow release of the Cur in the human plasma test, the formulation may be stable enough to facilitate the accumulation of pharmacologically active amounts of Cur in target cancer tissue by EPR. Therefore, our formulations could serve as a promising therapeutic approach for pancreatic cancer and other cancers.

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Section: Introductionmentioning

confidence: 99%

Long-Circulating Curcumin-Loaded Liposome Formulations with High Incorporation Efficiency, Stability and Anticancer Activity towards Pancreatic Adenocarcinoma Cell Lines In Vitro

et al. 2016

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“…The electrostatic and hydrogen interactions among the excipients thus provide biohybrid systems with improved properties, such as the delivery profile of active molecules increasing plasma halflife [83], permeation [84], and efficacy [85]. Furthermore, this combination of materials can be used to modulate viscosity, consistency, and mucoadhesion of lipid nanoparticles [86] or to add thermoreversible properties to the systems [87,88].…”

Section: Innovative Hybrid Lipid Nanoparticles: Solid Lipid Nanopartimentioning

confidence: 99%

“…The evaluation of transcorneal mechanism across the cornea was performed in rabbits, showing that the system allowed a prolonged residence time and reduced the systemic side effect. On the other hand, Hazzah et al [86] developed biohybrid sponges based on hydroxypropyl methylcellulose (HPMC) and polycarbophil as polymeric matrices, incorporating curcumin-loaded SLN for oral mucosal administration. The resulting materials showed a sustained delivery profile of curcumin and excellent mucoadhesion properties evaluated in five adult healthy volunteers.…”

Section: Innovative Hybrid Lipid Nanoparticles: Solid Lipid Nanopartimentioning

confidence: 99%

“…In vivo pharmacokinetics studies in rats demonstrated higher bioavailability of hybrid artesunateloaded lipospheres when compared to the commercial tablet for malaria treatment [104]. Different in vivo studies were described for SLN-and NLC-based hybrid systems for topical and parenteral applications, using mice, rat, and rabbit, as well as in human clinical trial, which demonstrated the effectiveness, nontoxicity, and bioavailability of these biodevices compared to their respective traditional DDS or free drug [86,88,94,96].…”

Section: In Vivo Performance Of Biohybrid Polymer-based Hybrid Ddsmentioning

confidence: 99%

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Advances in Hybrid Polymer-Based Materials for Sustained Drug Release

Ribeiro

Alcántara

Silva

et al. 2017

International Journal of Polymer Science

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The use of biomaterials composed of organic pristine components has been successfully described in several purposes, such as tissue engineering and drug delivery. Drug delivery systems (DDS) have shown several advantages over traditional drug therapy, such as greater therapeutic efficacy, prolonged delivery profile, and reduced drug toxicity, as evidenced by in vitro and in vivo studies as well as clinical trials. Despite that, there is no perfect delivery carrier, and issues such as undesirable viscosity and physicochemical stability or inability to efficiently encapsulate hydrophilic/hydrophobic molecules still persist, limiting DDS applications. To overcome that, biohybrid systems, originating from the synergistic assembly of polymers and other organic materials such as proteins and lipids, have recently been described, yielding molecularly planned biohybrid systems that are able to optimize structures to easily interact with the targets. This work revised the biohybrid DDS clarifying their advantages, limitations, and future perspectives in an attempt to contribute to further research of innovative and safe biohybrid polymer-based system as biomaterials for the sustained release of active molecules.

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“…Therefore, curcumin should be formulated in such a way that it can overcome these critical issues. In the current study, nanoformulations of curcumin have been designed with the aim of improving curcumin physicochemical and pharmacokinetic properties (7).…”

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confidence: 99%

Pharmacokinetic studies and anticancer activity of curcumin-loaded nanostructured lipid carriers

et al. 2017

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Pharmacokinetic studies and anticancer activity of curcumin-loaded nanostructured lipid carriersIn order to investigate the potential of nanostructured lipid carriers for efficient and targeted delivery of curcumin, the pharmacokinetic parameters of curcumin-loaded nanostructured lipid carriers (Cur-NLC) were evaluated in rats after a single intraperitoneal dose of Cur-NLC. In addition, the anticancer activity of Cur-NLC against human lung adenocarcinoma A549 cells was verified by a cellular uptake study, and a cytotoxicity and apoptosis assay. Bioavailability of Cur-NLC was better than that of native curcumin (p > 0.01), as seen from the area under the plasma concentration-time curve (AUC), maximum plasma concentration (C max) , mean residence time (MRT) and total plasma clearance (CL z /F).Cur-NLC has a more obvious lung-targeting property in comparison with native curcumin. Cur-NLC showed higher anticancer activity in vitro against A549 cells than native curcumin (IC 50 value of 5.66 vs. 9.81 mg L -1 , respectively). Meanwhile, Cur-NLC treated A549 cells showed a higher apoptosis rate compared to that of native curcumin. These results indicate that NLC is a promising system for the delivery of curcumin in the treatment of lung adenocarcinoma.Keywords: curcumin, nanostructured lipid carriers, pharmacokinetic, anticancer effects, lung adenocarcinoma Lung cancer is by far the most frequent cause of cancer-related deaths worldwide (1). The effectiveness of chemotherapeutic agents is often limited by the unavoidable toxicity of drug treatment. It is therefore essential to discover potential agents with more efficient therapeutic strategies and less severe side effects for the treatment of lung cancer. Phytochemicals have been gaining increasing attention as chemopreventive agents to treat various diseases, including lung cancer. Curcumin (C 21 H 20 O 6 ), a hydrophobic polyphenol, is an important phytochemical compound that gives the Asian spice turmeric its light yellow color. It is derived from the rhizome of Curcuma longa and has been long used as food color or for medication purposes worldwide, especially in India and other east Asian countries. 77 % curcumin I (diferuloylmethane), 17 % curcumin II (demethoxycurcumin) and 3 % curcumin III (bis-demethoxycurcumin) are the three major constituents of curcumin. Studies have indicated that curcumin has cancer preventive activity, either alone or in combination with other anticancer agents. Curcumin's widespread availability, safety, low cost and multiple cancer fighting functions make it a promising drug for the treatment of numerous cancers, including lung, cervical, breast, hepatic, pancreatic and colon cancer (2-5). The most attractive and vital reason for the therapeutic use of curcumin is its superior safety profile. It has been demonstrated that curcumin has very low toxicity, even at very high doses (6). Nevertheless, native curcumin cannot reach the therapeutic target in a therapeutic concentration because of its low bioavailability. Therefore, curcumin sho...

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Lyophilized sponges loaded with curcumin solid lipid nanoparticles for buccal delivery: Development and characterization

Cited by 76 publications

References 28 publications

Long-Circulating Curcumin-Loaded Liposome Formulations with High Incorporation Efficiency, Stability and Anticancer Activity towards Pancreatic Adenocarcinoma Cell Lines In Vitro

Long-Circulating Curcumin-Loaded Liposome Formulations with High Incorporation Efficiency, Stability and Anticancer Activity towards Pancreatic Adenocarcinoma Cell Lines In Vitro

Advances in Hybrid Polymer-Based Materials for Sustained Drug Release

Pharmacokinetic studies and anticancer activity of curcumin-loaded nanostructured lipid carriers

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