17 research outputs found

    Synthesis of novel polymeric nanoparticles (methoxy-polyethylene glycol-chitosan/hyaluronic acid) containing 7-ethyl-10-hydroxycamptothecin for colon cancer therapy: in vitro, ex vivo and in vivo investigation

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    The goal of the current study was to target 7-ethyl-10-hydroxycamptothecin (SN38) orally to colon tumours by synthesizing a targeting polymer. To achieve the optimum delivery for SN38, initially methoxy-polyethylene glycol (mPEG)-chitosan was synthesized and then nanoparticles were developed through ionic gelation between mPEG-chitosan and hyaluronic acid as a ligand for cell-surface glycoprotein CD44 receptor. The SN38 was loaded in nanoparticles (SN38-NPs) using the non-covalent physical adsorption method. The size of the optimized SN38-NPs was 226.7 nm, encapsulation efficiency was 89.23% and drug content was 7.98 ± 0.54% in the optimum formulation. The attachment of mPEG to chitosan was confirmed by proton nuclear magnetic resonance. The results of differential scanning calorimetry and Fourier transforms infra-red analysis indicated that SN38 existed in amorphous form and functional groups of SN38 protected in the formulations which could be a sign of suitable encapsulation of SN38 in SN38-NPs. In vitro study indicated that SN38-NPs were more potent against the cancer cells than free SN38. The cellular uptake of SN38-NPs improved up to 1.6-fold against human colorectal adenocarcinoma (Caco-2) cells. Moreover, SN38-NPs remarkably demonstrated superior anti-tumor efficacy in contrary to pure SN38. This suggests the advantage of SN38-NPs as a potent oral drug carrier which could be further explored for clinical investigations

    Encapsulation of nystatin in nanoliposomal formulation: characterization, stability study and antifungal activity against Candida albicans

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    In this study, nystatin liposomal formulation was prepared and characterized. The physicochemical properties of formulations including vesicle size, drug entrapment stability and in vitro release were studied. The highest entrapment efficiency of nystatin into liposomes was obtained about 70% when cholesterol (CHO) was added to the formulations prepared with dipalmitoylphosphatidylcholine. In addition, the drug entrapment efficiency was decreased when distearoylphosphatidylcholine was used   but it was improved by addition of CHO and hydration   with 9% sucrose solution. Liposomes with uniform size distribution and average size of 100 nm were produced.  Long term stability study indicated that the lyophilized liposomal nystatin was physically stable for at least 6 months at 4 °C. In vitro anti-fungal activity of liposomal nystatin was found to be more effective than free nystatin against Candida albicans

    Solid Dispersion Pellets: An Efficient Pharmaceutical Approach to Enrich the Solubility and Dissolution Rate of Deferasirox

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    Deferasirox (DFX) is an oral iron-chelating agent and classified into class II of the Biopharmaceutics Classification System. Low bioavailability of the drug due to insufficient solubility in physiological fluids is the main drawback of DFX. The idea of the current study was to explore the potential of solid dispersion (SD) as an effective method to improve the dissolution rate of DFX in pellets. The SDs were made by the solvent evaporation technique using polyethylene glycol 4000 (PEG 4000) and polyvinylpyrrolidone K25 with different drug-to-carrier ratios. Then, the dispersion was milled and mixed with other components and the mixture layered on sugar-based cores by pan coating technique. The pellets were evaluated in terms of size distribution, morphology (SEM), and dissolution behaviour. Drug-polymer interactions were studied using differential scanning calorimetry (DSC), X-ray diffraction study (XRD), and Fourier transformation infrared (FTIR) spectroscopy. The pellets coated with SD showed a remarkable rise in the solubility of DFX than that of free drug-loaded pellets. The dispersion with PVP K25 showed a faster dissolution rate as compared to other mixtures. The DSC and XRD analysis indicated that the drug was in the amorphous state when dispersed in the polymer. The FTIR studies demonstrated any ruled out interaction between drug and polymer. The SEM showed smoothness on the surface of the pellets. It is resolved that the SD method considerably enriched the dissolution rate of DFX in pellets, which can also be utilized for other poorly water-soluble drugs

    DNA-based Nanostructures as Novelty in Biomedicine

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    The application of nanocarriers in medicine and pharmaceuticals suggests a new procedure in nanotechnologyterminology, nanomedicine. DNA has been significantly highlighted due to its amazing functionality and natureas a nanomaterial in biomedicine. Given that DNA is biocompatible, its use as a nanomaterial in medicineprovides an excellent prospect for the rational engineering of DNA nanostructures. According to newapproaches in disease treatment at gene levels, gene therapy, DNA as a nanomedicine plays an essential role inthe medical sciences. In this field, researchers have published enormous documents regarding the applicationsof DNA and DNA-based nanostructures as drug or gene nanocarriers, DNA-based diagnostics, and DNA nanovaccines. In this review, the novelty of DNA-based nanomedicine has been considered

    Encapsulation of irinotecan in polymeric nanoparticles: Characterization, release kinetic and cytotoxicity evaluation

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    Objective(s): Irinotecan is a potent anti-cancer drug from camptothecin group which inhibits topoisomerase I. Recently, biodegradable and biocompatible polymers such as poly lactide-co-glycolides (PLGA) have been considered for the preparation of nanoparticles (NPs). Materials and Methods: In this study, irinotecan loaded PLGA NPs were fabricated by an emulsification/solvent diffusion method to improve the efficacy of irinotecan. The effect of several parameters on the NPs’ characteristics was assessed, including the amount of drug and polymer, the amount and volume of the poly vinyl alcohol as a surfactant, and also the internal-phase volume/composition. The irinotecan entrapment efficiency and the particle size distribution were optimized by changing these variables. The cytotoxicity of the particles was evaluated by cell viability assay.Results: NPs were spherical with a comparatively mono-dispersed size distribution and negative zeta potential. Selected formulation (S9) showed suitable size distribution about120 nm with relative high drug entrapment. MTT assay showed a stronger cytotoxicity of S9 against HT-29 cancer cells than control NPs and irinotecan free drug. The release kinetic indicated Log-Probability model in S9.Conclusion: Our results demonstrated that the designed NPs show suitable characteristic and also great potential for further in vivo cancer evaluation

    Enhancing osteogenic differentiation of dental pulp stem cells through rosuvastatin loaded niosomes optimized by Box-Behnken design and modified by hyaluronan: a novel strategy for improved efficiency

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    Abstract Bone tissue engineering necessitates a stem cell source capable of osteoblast differentiation and mineralized matrix production. Dental pulp stem cells (DPSCs), a subtype of mesenchymal stem cells from human teeth, present such potential but face challenges in osteogenic differentiation. This research introduces an innovative approach to bolster DPSCs’ osteogenic potential using niosomal and hyaluronan modified niosomal systems enriched with rosuvastatin. While rosuvastatin fosters bone formation by regulating bone morphogenetic proteins and osteoblasts, its solubility, permeability, and bioavailability constraints hinder its bone regeneration application. Using a Box-Behnken design, optimal formulation parameters were ascertained. Both niosomes were analyzed for size, polydispersity, zeta potential, and other parameters. They displayed average sizes under 275 nm and entrapment efficiencies exceeding 62%. Notably, niosomes boosted DPSCs’ cell viability and osteogenic marker expression, suggesting enhanced differentiation and bone formation. Conclusively, the study underscores the potential of both niosomal systems in ameliorating DPSCs’ osteogenic differentiation, offering a promising avenue for bone tissue engineering and regeneration. Graphical Abstrac
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