Lyophilized phytosomal nanocarriers as platforms for enhanced diosmin delivery: optimization and ex vivo permeation

Freag, May S.; Elnaggar, Yosra S.R.; Abdallah, Ossama Y.

doi:10.2147/ijn.s45231

Cited by 68 publications

(16 citation statements)

References 37 publications

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“…RSV in its natural state exists as crystals, which are characterized by the melting endothermic peak around 265 °C in its thermogram (Additional file 1: Figure S4A). The thermogram of RSV-PC complex demonstrated a broad peak at 281.567 °C, indicating a successful complexation between RSV and phosphatidylcholine [46, 47]. On the other hand, PMT thermogram demonstrated three characteristic peaks at 91.784, 153.818 and 243.8 °C [48].…”

Section: Resultsmentioning

confidence: 99%

Combining hydrophilic chemotherapy and hydrophobic phytotherapy via tumor-targeted albumin–QDs nano-hybrids: covalent coupling and phospholipid complexation approaches

et al. 2019

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BackgroundThe rationale of this study is to combine the merits of both albumin nanoparticles and quantum dots (QDs) in improved drug tumor accumulation and strong fluorescence imaging capability into one carrier. However, premature drug release from protein nanoparticles and high toxicity of QDs due to heavy metal leakage are among challenging hurdles. Following this platform, we developed cancer nano-theranostics by coupling biocompatible albumin backbone to CdTe QDs and mannose moieties to enhance tumor targeting and reduce QDs toxicity. The chemotherapeutic water soluble drug pemetrexed (PMT) was conjugated via tumor-cleavable bond to the albumin backbone for tumor site-specific release. In combination, the herbal hydrophobic drug resveratrol (RSV) was preformulated as phospholipid complex which enabled its physical encapsulation into albumin nanoparticles.ResultsAlbumin–QDs theranostics showed enhanced cytotoxicity and internalization into breast cancer cells that could be traced by virtue of their high fluorescence quantum yield and excellent imaging capacity. In vivo, the nanocarriers demonstrated superior anti-tumor effects including reduced tumor volume, increased apoptosis, and inhibited angiogenesis in addition to non-immunogenic response. Moreover, in vivo bioimaging test demonstrated excellent tumor-specific accumulation of targeted nanocarriers via QDs-mediated fluorescence.ConclusionMannose-grafted strategy and QD-fluorescence capability were beneficial to deliver albumin nanocarriers to tumor tissues and then to release the anticancer drugs for killing cancer cells as well as enabling tumor imaging facility. Overall, we believe albumin–QDs nanoplatform could be a potential nano-theranostic for bioimaging and targeted breast cancer therapy.Electronic supplementary materialThe online version of this article (10.1186/s12951-019-0445-7) contains supplementary material, which is available to authorized users.

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Section: Resultsmentioning

confidence: 99%

Combining hydrophilic chemotherapy and hydrophobic phytotherapy via tumor-targeted albumin–QDs nano-hybrids: covalent coupling and phospholipid complexation approaches

et al. 2019

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“…The dissolution profile of the CN followed a near zero-order release, and at the end of 12 h, over 99% w/w SCE was observed to be released from the CN. The dissolution rate is largely influenced by the crystal morphology and the wettability of the solids, and the improved dissolution rate of SCE from the CN may be explained by the improved solubility, and the partially disrupted crystalline phase (amorphous form) in the prepared naturosome (5,50). The relatively higher amorphous state of the naturosome, and their increased water-solubility may have had a positive impact on the cumulative release of the drug.…”

Section: In Vitro Drug Release (Dissolution)mentioning

confidence: 99%

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Saoji

Raut

Dhore

et al. 2015

AAPS J

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Abstract. In the present study, a phospholipid-based complex of standardized Centella extract (SCE) was developed with a goal of improving the bioavailability of its phytoconstituents. The SCE-phospholipid complex was prepared by solvent evaporation method and characterized for its physicochemical and functional properties. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), photomicroscopy, and powder x-ray diffraction (PXRD) were used to confirm the formation of Centella naturosome (CN). The prepared complex was functionally evaluated by apparent solubility, in vitro drug release, ex vivo permeation, and in vivo efficacy studies. The prepared CN exhibited a significantly higher (12-fold) aqueous solubility (98.0±1.4 μg/mL), compared to the pure SCE (8.12±0.44 μg/mL), or the physical mixture of SCE and the phospholipid (13.6±0.4 μg/mL). The in vitro dissolution studies revealed a significantly higher efficiency of CN in releasing the SCE (99.2±4.7, % w/w) in comparison to the pure SCE (39.2±2.3, % w/w), or the physical mixture (42.8±2.09, % w/w). The ex vivo permeation studies with the everted intestine method showed that the prepared CN significantly improved the permeation of SCE (82.8±3.7, % w/w), compared to the pure SCE (26.8±2.4, % w/w), or the physical mixture (33.0±2.7, % w/w). The in vivo efficacy studies using the Morris Water Maze test indicated a significant improvement of the spatial learning and memory in aged mice treated with CN. Thus, drug-phospholipid complexation appears to be a promising strategy to improve the aqueous solubility and bioavailability of bioactive phytoconstituents.

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“…The amount of drug permeation was estimated by UV-visible spectrophotometer as described above. The permeability of CFX was calculated by utilizing a plot of cumulative CFX permeation across the duodenum verses time [ 54 ]. Furthermore, apparent permeability was calculated by using following formula, P app = Q/Act where P app is permeability coefficient, Q (mg)= total amount permeated through intestine, A (cm 2 ) = surface area of permeation surface, C (mg/cm 3 ) = initial concentration of drug, t = total time of permeation study.…”

Section: Methodsmentioning

confidence: 99%

Enhanced Intestinal Permeability of Cefixime by Self-Emulsifying Drug Delivery System: In-Vitro and Ex-Vivo Characterization

et al. 2023

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Background: Cefixime (CFX) belongs to a group of third-generation cephalosporin antibiotics with low water solubility and low intestinal permeability, which ultimately leads to significantly low bioavailability. Aim: This study aimed to increase solubility, improve drug release, and intestinal permeability of CFX by loading into SEDDS. Methods: Suitable excipients were selected based on drug solubility, percent transmittance, and emulsification efficiency. Pseudo-ternary phase diagram was fabricated for the identification of effective self-emulsification region. The best probably optimized formulations were further assessed for encumbered drug contents, emulsification time, cloud point measurement, robustness to dilution, mean droplet size, zeta potential, polydispersity index (PDI), and thermodynamic and chemical stability. Moreover, in vitro drug release studies and ex vivo permeation studies were carried out and apparent drug permeability Papp of different formulations was compared with the marketed brands of CFX. Results: Amongst the four tested SEDDS formulations, F-2 formulation exhibited the highest drug loading of 96.32%, emulsification time of 40.37 ± 3 s, mean droplet size of 19.01 ± 1.12 nm, and demonstrated improved long-term thermodynamic and chemical stability when stored at 4 °C. Release studies revealed a drug release of 97.32 ± 4.82% within 60 min in simulated gastric fluid. Similarly, 97.12 ± 5.02% release of CFX was observed in simulated intestinal fluid within 120 min; however, 85.13 ± 3.23% release of CFX was observed from the marketed product. Ex vivo permeation studies displayed a 2.7-fold increase apparent permeability compared to the marketed product in 5 h. Conclusion: Owing to the significantly improved drug solubility, in vitro release and better antibacterial activity, it can be assumed that CFX-loaded SEDDS might lead to an increased bioavailability and antibacterial activity, possibly leading to improved therapeutic effectiveness.

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Lyophilized phytosomal nanocarriers as platforms for enhanced diosmin delivery: optimization and ex vivo permeation

Cited by 68 publications

References 37 publications

Combining hydrophilic chemotherapy and hydrophobic phytotherapy via tumor-targeted albumin–QDs nano-hybrids: covalent coupling and phospholipid complexation approaches

Combining hydrophilic chemotherapy and hydrophobic phytotherapy via tumor-targeted albumin–QDs nano-hybrids: covalent coupling and phospholipid complexation approaches

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Enhanced Intestinal Permeability of Cefixime by Self-Emulsifying Drug Delivery System: In-Vitro and Ex-Vivo Characterization

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