Enhancement of zaleplon oral bioavailability using optimized self-nano emulsifying drug delivery systems and its effect on sleep quality among a sample of psychiatric patients

Khalifa, Maha K A; Salem, Hoda A.; Shawky, Seham; Eassa, Heba A.; Elaidy, Asmaa M.

doi:10.1080/10717544.2019.1687613

Cited by 18 publications

(10 citation statements)

References 35 publications

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“…The excess liquid was then removed with absorbent paper. Prior to inspection with an acceleration voltage of 70 kV and magnification power of 150 KX 19, the sample was stained with a drop of an aqueous solution of phosphotungstic acid (2% w/v) for 3 min (2 % w/v) for 3 minutes [20] .…”

Section: Transmission Electron Microscopy (Tem)mentioning

confidence: 99%

Trifluoperazine-Loaded Leciplexes as Potential Nasal Delivery Systems for treatment of depression

Refai

Osman

Khalifa

et al. 2022

Azhar International Journal of Pharmaceutical and Medical Scien

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Trifluoperaizne (TFP) is an antipsychotic medication with limited oral bioavailability due to extensive first-pass metabolism; consequently, the goal of this project was to develop Leciplex nanoparticles to improve the bioavailability of TFP and to prolong its nasal residence time for treatment of the depression. Leciplex NPs were prepared using negatively charged phospholipid, cationic surfactant and biocompatible solvent and optimized using the 21 31 full factorial statistical design using various surfactants and different phospholipid to surfactant ratios. Design Expert® software was employed to select the optimum formula. The formulae were characterized regarding their particle size (PS), polydispersity index (PDI), zeta potential (ZP), entrapment efficiency percentages (EE %), amount of drug released after 6 hours (Q6h), transmission electron microscopy analysis, fourier transform infrared ray spectroscopy (FT-IR) and stability for six months. Optimized formula was contained dimethyldidodecylammonium bromide as surfactant and had a

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Section: Transmission Electron Microscopy (Tem)mentioning

confidence: 99%

Trifluoperazine-Loaded Leciplexes as Potential Nasal Delivery Systems for treatment of depression

Refai

Osman

Khalifa

et al. 2022

Azhar International Journal of Pharmaceutical and Medical Scien

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“…Extra fluid was then eliminated by with the aid of an absorbent paper, then observed by TEM (JEM 1010, JEOL Ltd, Tokyo, Japan) with an acceleration voltage of 70kV and magnification power of 150 KX. 29 , 30 …”

Section: Methodsmentioning

confidence: 99%

Investigating the Impact of Optimized Trans-Cinnamic Acid-Loaded PLGA Nanoparticles on Epithelial to Mesenchymal Transition in Breast Cancer

Badawi¹,

Attia²,

El‐Kersh³

et al. 2022

IJN

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Purpose To design and optimize trans -cinnamic acid-loaded PLGA nanoparticles (CIN-PLGA-NPs) and assess its inhibitory effect on epithelial-mesenchymal transition (EMT) in triple-negative breast cancer. Methods The quality by design approach was used to correlate the formulation parameters (PLGA amount and Poloxamer188 concentration) and critical quality attributes (entrapment efficiency percent, particle size and zeta potential). Design of CIN-PLGA-NPs formulations was done based on central composite response surface design and formulated by nanoprecipitation method. In addition, the optimized CIN-PLGA-NPs formulation was further evaluated for morphology using transmission electron microscopy and in vitro dissolution test. The cytotoxicity of CIN-PLGA-NPs optimized formula in comparison to the free trans -cinnamic acid (CIN-Free) was investigated in vitro using MDA-MB-231, triple-negative breast cancer cells, followed by scratch wound assay for evaluating the impact on the migratory potential of MDA-MB-231 cells. In vivo antitumor activity was evaluated using Ehrlich ascites carcinoma solid tumor animal model where tumor volumes were measured at different time points and necrotic/apoptotic indices were estimated in tumor sections. EMT markers, E- and N-cadherin, were assessed in solid tumors as well. Results The optimized formulation showed entrapment efficiency of 76.98%, particle size of 186.3 nm with a smooth spherical surface and zeta potential of −28.47 mV indicating its stability. Furthermore, CIN-PLGA-NPs optimized formula released 60.8±1.89% of the total CIN-Free within 24 hours compared to 29±1.25% of the raw CIN-Free indicating improved dissolution rate. The optimized formula showed superior cytotoxicity on MDA-MB-231 cells compared to its free counterpart as well as increased wound closure percentage along with reduced tumor size in mice and increased necrotic and apoptotic indices. Tumor levels of E-cadherin and N-cadherin were indicative of EMT inhibition. Conclusion Our findings proved the capability of PLGA nanoparticles in loading trans -cinnamic acid in addition to enhancing its antitumor efficacy in triple-negative breast cancer possibly via inhibiting EMT.

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“…A small number of SEDDS-based products have already been successfully introduced into the pharmaceutical market, with none of them loading drugs for the treatment of neurological disorders. Until now, several in vivo assays using oral SEDDS have been carried out for neuropharmaceuticals brain targeting [ 4 , 6 , 23 , 24 , 25 , 29 , 30 , 31 , 32 , 33 , 34 , 35 , 36 , 37 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 70 ], but only a few in vivo pre-clinical studies have been reported for IN administration of neurotherapeutics loaded in SEDDS. In fact, only six studies were found that investigated the IN administration of neurotherapeutics loaded in SEDDS: clonazepam [ 45 ], diazepam [ 44 ], and perampanel [ 28 ] for epilepsy treatment; Bdph for glioblastoma treatment [ 4 ]; huperzine A [ 30 ] for Alzheimer’s disease; and naringin [ 5 ] as a neuroprotective for Alzheimer’s and Parkinson’s disease.…”

Section: Application Of Sedds In Brain Drug Delivery—pre-clinical Stu...mentioning

confidence: 99%

Self-Emulsifying Drug Delivery Systems: An Alternative Approach to Improve Brain Bioavailability of Poorly Water-Soluble Drugs through Intranasal Administration

2022

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Efforts in discovering new and effective neurotherapeutics are made daily, although most fail to reach clinical trials. The main reason is their poor bioavailability, related to poor aqueous solubility, limited permeability through biological membranes, and the hepatic first-pass metabolism. Nevertheless, crossing the blood–brain barrier is the major drawback associated with brain drug delivery. To overcome it, intranasal administration has become more attractive, in some cases even surpassing the oral route. The unique anatomical features of the nasal cavity allow partial direct drug delivery to the brain, circumventing the blood–brain barrier. Systemic absorption through the nasal cavity also avoids the hepatic first-pass metabolism, increasing the systemic bioavailability of highly metabolized entities. Nevertheless, most neurotherapeutics present physicochemical characteristics that require them to be formulated in lipidic nanosystems as self-emulsifying drug delivery systems (SEDDS). These are isotropic mixtures of oils, surfactants, and co-surfactants that, after aqueous dilution, generate micro or nanoemulsions loading high concentrations of lipophilic drugs. SEDDS should overcome drug precipitation in absorption sites, increase their permeation through absorptive membranes, and enhance the stability of labile drugs against enzymatic activity. Thus, combining the advantages of SEDDS and those of the intranasal route for brain delivery, an increase in drugs’ brain targeting and bioavailability could be expected. This review deeply characterizes SEDDS as a lipidic nanosystem, gathering important information regarding the mechanisms associated with the intranasal delivery of drugs loaded in SEDDS. In the end, in vivo results after SEDDS intranasal or oral administration are discussed, globally revealing their efficacy in comparison with common solutions or suspensions.

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Enhancement of zaleplon oral bioavailability using optimized self-nano emulsifying drug delivery systems and its effect on sleep quality among a sample of psychiatric patients

Cited by 18 publications

References 35 publications

Trifluoperazine-Loaded Leciplexes as Potential Nasal Delivery Systems for treatment of depression

Trifluoperazine-Loaded Leciplexes as Potential Nasal Delivery Systems for treatment of depression

Investigating the Impact of Optimized Trans-Cinnamic Acid-Loaded PLGA Nanoparticles on Epithelial to Mesenchymal Transition in Breast Cancer

Self-Emulsifying Drug Delivery Systems: An Alternative Approach to Improve Brain Bioavailability of Poorly Water-Soluble Drugs through Intranasal Administration

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