DOE, formulation, and optimization of Repaglinide nanostructured lipid carriers

Swidan, Shady; Mansour, Zeinab N.; Mourad, Zeinab A.; Elhesaisy, Nahla A.; Khaled, Rehab; Bekheet, Mohamed S.; Badawy, Mohamed A.; Elsemeiri, Mai M.; Elrefaey, Aya E.; Hassaneen, Amera M.

doi:10.7324/japs.2018.81002

Cited by 22 publications

(6 citation statements)

References 27 publications

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“…It was stated in other studies that the presence of a solid lipid reduces the ζ potential values. It was also reported that there are ζ levels higher than SLNs, especially in preparations in the form of emulsions prepared with liquid lipids. − …”

Section: Results and Discussionmentioning

confidence: 99%

Co-Delivery of siRNA and Docetaxel to Cancer Cells by NLC for Therapy

Şenel,

Başaran,

Akyıl

et al. 2024

ACS Omega

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The present study aims to develop a delivery system that can carry small interference RNA (siRNA) with smallmolecule chemotherapeutic drugs, which can be used in cancer treatment. The drug delivery system combines the advantages of a therapeutic agent with two different mechanisms to ensure that it is used efficiently for cancer therapy. In this study, a nanostructured lipid carrier system was prepared, Docetaxel was loaded to these systems, and the Eph siRNA was adsorbed to the outer surface. In addition, DOTAP was added to the lipophilic phase to load a positive charge on the lipidic structure for interaction with the cells. Moreover, characterization, cytotoxicity, and transfection procedures were performed on the whole system. This candidate system was also compared to Taxotere, which is the first approved Docetaxel-containing drug on the market. Given the results, it was determined that the particle size of NLC-DTX was 165.3 ± 3.5 nm, the ζ potential value was 38.2 ± 1.7 mV, and the PDI was 0.187 ± 0.024. Entrapment efficacy of nanoparticles was found to be 92.89 ± 0.21%. It was determined that the lipidic system prepared in vitro release analyses were able to provide sustained release and exhibit cytotoxicity, even at doses lower than the dose used for Taxotere. The formulations prepared had a higher level of effect on cells when compared with pure DTX and Taxotere, but they also exhibited time-dependent cytotoxicity. It was also observed that the use of Eph siRNA together with the chemotherapeutic agent via formulation also contributed to this cell death. The results of the present study indicate that there is a promising carrier system in order to deliver hydrophilic nucleic acids, such as siRNA, together with lipophilic drugs in cancer treatment.

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Section: Results and Discussionmentioning

confidence: 99%

Co-Delivery of siRNA and Docetaxel to Cancer Cells by NLC for Therapy

Şenel,

Başaran,

Akyıl

et al. 2024

ACS Omega

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“…The slower later release came from Apx was integrated into the NLC core and released in a sustained pattern through the matrix erosion or degradation. In contrast, the faster initial release came from Apx, rapidly diffusing from the surface [ 76 , 77 ]. Compared to the free Apx, it was clear that the optimized formula showed a slower release.…”

Section: Resultsmentioning

confidence: 99%

Tailoring Apixaban in Nanostructured Lipid Carrier Enhancing Its Oral Bioavailability and Anticoagulant Activity

et al. 2022

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Apixaban (Apx), an oral anticoagulant drug, is a direct factor Xa inhibitor for the prophylaxis against venous thromboembolism. Apx has limited oral bioavailability and poor water solubility. The goal of this study was to improve the formulation of an Apx-loaded nanostructured lipid carrier (NLC) to increase its bioavailability and effectiveness. As solid lipid, liquid lipid, hydrophilic, and lipophilic stabilizers, stearic acid, oleic acid, Tween 80, and lecithin were used, respectively. Utilizing Box–Behnken design, the effects of three factors on NLC particle size (Y1), zeta potential (Y2), and entrapment efficiency percent (Y3) were examined and optimized. The optimized formula was prepared, characterized, morphologically studied, and pharmacokinetically and pharmacodynamically assessed. The observed responses of the optimized Apx formula were 315.2 nm, −43.4 mV, and 89.84% for Y1, Y2, and Y3, respectively. Electron microscopy revealed the homogenous spherical shape of the NLC particles. The in vivo pharmacokinetic study conducted in male Wistar rats displayed an increase in AUC and Cmax by 8 and 2.67 folds, respectively, compared to oral Apx suspension. Moreover, the half-life was increased by 1.94 folds, and clearance was diminished by about 8 folds, which makes the NLC formula a promising sustained release system. Interestingly, the pharmacodynamic results displayed the superior effect of the optimized formula over the drug suspension with prolongation in the cuticle bleeding time. Moreover, both prothrombin time and activated partial thromboplastin time are significantly increased. So, incorporating Apx in an NLC formula significantly enhanced its oral bioavailability and pharmacodynamic activity.

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“…The DSC thermograms of pure GMS, SIM powder, and lyophilized NLC.1 are shown in figure 6. The pure GMS and SIM exhibit a sharp endothermic peak at 69.13 • C and 142.93 • C, respectively, which are attributed to the melting of the samples [39,67]. The thermogram of lyophilized NLC.1 shows an endothermic peak at 55.59 • C which is significantly (P < 0.05) different compared to the melting peak of pure lipid.…”

Section: Dsc Analysismentioning

confidence: 90%

Synthesis and characterization of a novel hydrogel based on carboxymethyl chitosan/sodium alginate with the ability to release simvastatin for chronic wound healing

Karami

Saber‐Samandari

2023

Biomed. Mater.

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Since wound dressing has been considered a promising strategy to improve wound healing, recent attention has been focused on the development of modern wound dressings based on synthetic and bioactive polymers. In this study, we prepared a multifunctional wound dressing based on carboxymethyl chitosan/sodium alginate hydrogel containing a nanostructured lipid carrier in which simvastatin has been encapsulated. This dressing aimed to act as a barrier against pathogens, eliminate excess exudates, and accelerate wound healing by increasing the production of vascular endothelial growth factor (VEGF). Among various fabricated composites of dressing, the hydrogel composite with a carboxymethyl chitosan/sodium alginate ratio of 1:2 had an average pore size of about 98.44 ± 26.9 μm and showed 707 ± 31.9 % swelling and a 2116 ± 79.2 g/m2.per day water vapor transfer rate (WVTR), demonstrating appropriate properties for absorbing exudates and maintaining wound moisture. The nanostructured lipid carrier with optimum composition and properties had a spherical shape and uniform particle size distribution (74.46 ±7.9 nm). The prepared nanocomposite hydrogel displayed excellent antibacterial activity against Escherichia coli and Staphylococcus aureus bacteria as well as high biocompatibility on L929 mouse fibroblast cells. It can release the loaded simvastatin drug slowly and over a prolonged period of time. The highest drug release occurred (80%) within 14 days. The results showed that this novel nanocomposite could be a promising candidate as a wound dressing for treating various chronic wounds in skin tissues.

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DOE, formulation, and optimization of Repaglinide nanostructured lipid carriers

Cited by 22 publications

References 27 publications

Co-Delivery of siRNA and Docetaxel to Cancer Cells by NLC for Therapy

Co-Delivery of siRNA and Docetaxel to Cancer Cells by NLC for Therapy

Tailoring Apixaban in Nanostructured Lipid Carrier Enhancing Its Oral Bioavailability and Anticoagulant Activity

Synthesis and characterization of a novel hydrogel based on carboxymethyl chitosan/sodium alginate with the ability to release simvastatin for chronic wound healing

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