Ex-Vivo Absorption Study of a Novel Dabigatran Etexilate Loaded Nanostructured Lipid Carrier Using Non-Everted Intestinal Sac Model

Abed, haithem N; Hussein, Ahmed A.

doi:10.31351/vol28iss2pp37-45

Cited by 8 publications

(7 citation statements)

References 23 publications

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“…Formula 1: Cold homogenization was used to create GCV-NLCs, and the following technique was used with slight changes. 6 The solid lipid PA and OA as a liquid lipid were melted, then 1% transcutol was added as a solubilizer and mixed into the melted lipid. Finally, 75 mg of GCV was added, and the mixture was magnetically stirred for two minutes.…”

Section: Preparation Of Drug-loaded Nlcmentioning

confidence: 99%

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Improvement of Entrapment and Ocular Permeability of Ganciclovir Nanostructured Lipid Carriers Using Various Conditions of Preparations

Salih¹,

Al-Gawhari²

2023

IJDDT

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Ganciclovir (GCV) is a drug included in BCS-Class III, having high solubility and low permeability. It is a synthetic acyclic nucleoside analog of 2′-deoxyguanosine, considered a potent inhibitor of herpes viruses and cytomegalovirus (CMV) infection. Herpes simplex virus (HSV) infections are very common and are also considered a major cause of corneal blindness. This study intended to advance a pioneering nanostructured lipid carriers (NLCs) system for improving the ocular permeability of GCV. Several procedures were used for the preparation. Cold homogenization, solvent injection, and emulsifi cationultrasonication methods. A mixture of palmitic acid (PA) and oleic acid (OA) as a lipid matrix, cremophore EL, and transcutol HP were used as emulsifi ers. To evaluate the optimum method, the particle size (PS), polydispersity index (PDI), zeta potential (ZP), entrapment effi ciency (EE), and drug loading (DL%) were determined for the prepared NLCs. Due to the decreased particle size value, the polydispersity index, and the high value of EE%, emulsifi cation/ultrasonication outcomes were more practical than cold homogenization and solvent injection procedures. The fi ndings demonstrated that the preparation procedure had a substantial impact on the EE%.The emulsifi cation method can prepare the NLCs of GCV successfully.

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Section: Preparation Of Drug-loaded Nlcmentioning

confidence: 99%

“…After the materials were diluted with double-distilled water, the particle means diameter and PDI measurements were made. 6…”

Section: Particle Size (Ps) and Poly Dispersity Index (Pdi) Determina...mentioning

confidence: 99%

Improvement of Entrapment and Ocular Permeability of Ganciclovir Nanostructured Lipid Carriers Using Various Conditions of Preparations

Salih¹,

Al-Gawhari²

2023

IJDDT

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“…The hydrodynamic diameters and size distribution (polydispersity index) of sHDL were determined by dynamic light scattering system (DLS) using a 90Plus Particle Size Analyzer (Brookhaven Instruments Corporation, USA). Each sample was diluted with equal volume of distilled water (DW), and analyzed at temperature of 25⁰C (18) .…”

Section: Characterization Of Shdl Nanoparticles Determination Of Part...mentioning

confidence: 99%

Preparation and in vitro evaluation of synthetic high-density lipoproteins as parenteral drug delivery system for tamoxifen citrate

Radhi,

Ali,

Al-Saedi

2023

IJPS

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The aim of this study was to develop a bioinspired drug delivery system for tamoxifen citrate (TC) based on synthetic high density lipoproteins (sHDL). For this purpose, sHDL nanoparticles were prepared from a mimetic peptide (5A peptide) and different lipids using thin film hydration method followed by sonication and thermal cycling. Various formulation parameters including lipid composition, lipid to peptide ratio, and drug to carrier ratio had a remarkable impact on the properties and the release pattern of the nanoparticles. The optimized formula (F14) displayed a spherical morphology, average diameter of (35.7±12.4) nm, and a zeta potential (ζ) equals to (-48.4± 0.5) mV. The encapsulation efficiency and drug loading of F14 were (96.5±0.7%) and (9.65±0.1%), respectively. Besides, F14 showed a good stability in human plasma for 24 hours. The encapsulation of the lipophilic drug within the hydrophobic core of the nanocarrier enabled a slow drug release from nanoparticles which follows a near zero order controlled mechanism. The promising results of this study opens an avenue for using sHDL as a delivery system for administration of TC intravenously. Therefore, the optimized formula is suggested to be subject for future analyses in terms of in vitro cytotoxicity against breast cancer cells and in vivo evaluation in tumor bearing animals.

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“…Ex vivo study was achieved on fasted male sheep weighing about 16 kg using the non-everted sac method. [32][33][34] The animal slay and anatomize according to the legal method achieved in the university of Baghdad/ college of pharmacy. The small intestine was isolated and carefully removed mesentery matter and washed the small intestine by cold normal saline solution.…”

Section: Ex-vivo Intestinal Permeation Studymentioning

confidence: 99%

“…It was observed that the pure drug suspension gives a lower permeation coefficient in comparison to all optimized felodipine LPHNs formulations(F1-F9) because that felodipine LPHNs formulations belong to lipid base nanosystem that increases solubility and intestinal permeation also, nanoscale of these hybrid carriers provide large surface area for molecular felodipine libration and rapid absorption to the systemic circulation. [32][33][34] The analysis of variance indicates a significant(p-value <0.05) correlation between the blend of PEG laurate: polysorbate 80: propylene glycol contents, lipid content, and chitosan polymer and ex vivo intestinal permeation parameter.…”

Section: Ex-vivo Intestinal Permeation Studymentioning

confidence: 99%

Lipid-Polymer Hybrid Nanocarriers for Oral Delivery of Felodipine: Formulation, Characterization and Ex-Vivo Evaluation

Drais

Abbas

2021

Adv Pharm Bull

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Purpose: Felodipine, is a calcium-channel antagonist used for hypertension and angina pectoris. It is practically insoluble in aqueous media and shows low oral bioavailability (15%-20%). This investigation aims to prepare and characterize oral felodipine lipid-polymer hybrid nanocarriers (LPHNs) to increase solubility and control delivery for increasing bioavailability and enhance patient compliance. Methods: The newly microwave-based method was prepared with felodipine LPHNs (H1-H35) successfully. The (H1-H35) were subjected to thermodynamic stability experiments. After that, select nine felodipine LPHNs (F1-F9) that have smart physical stability for further optimization of different characterization processes. Results: The felodipine LPHNs (F4) are considered the most optimized formula. It was characterized by lower particle size (33.3 nm), lower PDI (0.314), high zeta potential (13.6 mV), entrapment efficiency is (81.645 %w/w), drug loading is (16.329 % w/w), the pH value is 4, excellent percent of light transmittance (95.5%), pseudoplastic rheogram, significantly high (p< 0.05) dissolution rate with sustained drug delivery and success ex-vivo intestinal permeation attributes. The (F4) subject for further investigations of fourier transformed infrared spectroscopy (FTIR), atomic force microscopy (AFM), and transmission electron microscopy (TEM). The results of FTIR, AFM, and TEM indicate there is no interaction between the felodipine and excipients and that the particulate system in the nanoscale dispersion system confirms the high stability. Conclusion: The optimized felodipine LPHNs (F1-F9) formulations were smart formulations for sustained oral delivery of felodipine and that F4 was the most optimized formula according to its characterization processes.

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Ex-Vivo Absorption Study of a Novel Dabigatran Etexilate Loaded Nanostructured Lipid Carrier Using Non-Everted Intestinal Sac Model

Cited by 8 publications

References 23 publications

Improvement of Entrapment and Ocular Permeability of Ganciclovir Nanostructured Lipid Carriers Using Various Conditions of Preparations

Improvement of Entrapment and Ocular Permeability of Ganciclovir Nanostructured Lipid Carriers Using Various Conditions of Preparations

Preparation and in vitro evaluation of synthetic high-density lipoproteins as parenteral drug delivery system for tamoxifen citrate

Lipid-Polymer Hybrid Nanocarriers for Oral Delivery of Felodipine: Formulation, Characterization and Ex-Vivo Evaluation

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