scholarly journals Preparation and Evaluation of Carbamazepine Solid Lipid Nanoparticle for Alleviating Seizure Activity in Pentylenetetrazole-Kindled Mice

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3971 ◽  
Author(s):  
Mona Qushawy ◽  
Kousalya Prabahar ◽  
Mohammed Abd-Alhaseeb ◽  
Shady Swidan ◽  
Ali Nasr
Keyword(s):  
Histopathological Examination ◽  
In Vitro Release ◽  
Aqueous Dispersion ◽  
Entrapment Efficiency ◽  
Anticonvulsant Effect ◽  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Lipid Nanoparticle

Objectives: The study aimed to prepare carbamazepine in solid lipid nanoparticle form (CBZ-SLN) in order to enhance its anticonvulsant effect. Method: Eight formulations of CBZ-SLNs were prepared by homogenization and ultra-sonication techniques. Results: The prepared CBZ-SLN showed a high entrapment efficiency% (39.66 ± 2.42%–71.91 ± 1.21%), a small particle size (45.11 ± 6.72–760.7 ± 5.25 nm), and a negative zeta potential (from −21.5 ± 1.02 to −38.4 ± 1.32 mv). The in vitro release study showed the slow release of CBZ from SLNs compared to CBZ aqueous dispersion (p < 0.05). The infrared spectroscopy and the thermal analysis revealed the compatibility of the drug with other ingredients and the presence of drug in the more soluble amorphous estate, respectively. The in vivo study on mice revealed that the CBZ-SLN had a higher anticonvulsant efficacy than CBZ aqueous dispersion after a lethal and chronic dose of pentylenetetrazole (PTZ) (p < 0.05). The histopathological examination of the hippocampus revealed a decrease in the percentage of degeneration in mice treated with the CBZ-SLN compared to the PTZ and CBZ groups. Conclusion: CBZ can be formulated as SLN with higher anticonvulsant activity than free CBZ aqueous dispersion.

scholarly journals Solid lipid nanoparticle induced apoptosis of macrophages via a mitochondrial-dependent pathway in vitro and in vivo

2019 ◽  
Vol Volume 14 ◽  
pp. 3283-3295 ◽  
Author(s):  
Wan-Li Liang ◽  
Lan Xiao ◽  
Hong-Wei Gu ◽  
Xiao-Jun Li ◽  
Yu-Sang Li ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Lipid Nanoparticle ◽  
Induced Apoptosis ◽  
Dependent Pathway

Application of Novel Solid Lipid Nanoparticle (SLN)-Gene Vector Formulations Based on a Dimeric HIV-1 TAT-Peptide in Vitro and in Vivo

2004 ◽  
Vol 21 (9) ◽  
pp. 1662-1669 ◽  
Author(s):  
Carsten Rudolph ◽  
Ulrike Schillinger ◽  
Aurora Ortiz ◽  
Kerstin Tabatt ◽  
Christian Plank ◽  
...  
Keyword(s):  
Gene Vector ◽  
Tat Peptide ◽  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Lipid Nanoparticle ◽  
Hiv 1

scholarly journals Solid Lipid Nanoparticle Formulations of Docetaxel Prepared with High Melting Point Triglycerides: In Vitro and in Vivo Evaluation

2014 ◽  
Vol 11 (4) ◽  
pp. 1239-1249 ◽  
Author(s):  
Youssef Wahib Naguib ◽  
B. Leticia Rodriguez ◽  
Xinran Li ◽  
Stephen D. Hursting ◽  
Robert O. Williams ◽  
...  
Keyword(s):  
Melting Point ◽  
High Melting ◽  
Solid Lipid Nanoparticle ◽  
High Melting Point ◽  
In Vivo Evaluation ◽  
Solid Lipid ◽  
Lipid Nanoparticle

scholarly journals OCULAR DELIVERY OF NATAMYCIN SOLID LIPID NANOPARTICLE LOADED MUCOADHESIVE GEL: FORMULATION, CHARACTERIZATION AND IN VIVO STUDY

2020 ◽  
pp. 173-180
Author(s):  
REHAB ABDELMONEM ◽  
MOHAMED A. EL-NABARAWI ◽  
ALSHIMAA M. ATTIA ◽  
MAHMOUD TEAIMAA
Keyword(s):  
Controlled Release ◽  
Histopathological Examination ◽  
Hydroxypropyl Methylcellulose ◽  
Experimental Studies ◽  
Pluronic F127 ◽  
In Vivo Study ◽  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Lipid Nanoparticle

Objective: This study aimed to develop a novel topical ocular system of natamycin (NAT) by formulating and evaluating of NAT-solid lipid nanoparticle (SLN) loaded on mucoadhesive gels to improve its therapeutic activity and reduce the frequency of dosage to assist patient compliance. Methods: SLNs were prepared using lipids and Tween 80 or Pluronic F127 as stabilizers via modified high shear homogenization and ultrasound techniques. The prepared SLNs were characterized for particle size (PS), zeta potential (ZP), polydispersity index (PI), and entrapment efficiency percentage (EE %). The morphological examination for chosen SLNs was done using a transmission electron microscope (TEM). Carbapol 940 and Hydroxypropyl methylcellulose (HPMC) was incorporated with selected NAT-SLNs to form mucoadhesive gels. The prepared NAT-SLN gels were evaluated for drug content, mucoadhesion force, release study, and in vitro microbiological activity. In vivo study for the chosen formulae was done to evaluate its efficacy against keratitis in rabbits. Results: NAT-SLNs exhibited high EE % up to 99.167% and PS ranging from 128.35 to 1719.5 nm, with negatively charged ZP that confirmed the stability of SLNs. The NAT-SLN gels provided the high mucoadhesive force with a controlled release manner compared with the marketed-product MP. The in vivo experimental studies and histopathological examination showed the superiority of G2 (NAT-SLN (5% Pluronic F127 and 1:1 mixed lipid) 4% HPMC) over MP against Candida keratitis. Conclusion: According to the obtained results, G2 provided an effective pharmaceutical system against fungal keratitis in a controlled release manner compared with MP for reducing dosage frequency.

Preparation, Characterization and in vivo Evaluation of Felodipine Solid-Lipid Nanoparticles for Improved Oral Bioavailability

2015 ◽  
Vol 8 (4) ◽  
pp. 2995-3002
Author(s):  
Kishan V ◽  
Usha Kiranmai Gondrala ◽  
Narendar Dudhipala
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation ◽  
Solid Lipid

Felodipine is an antihypertensive drug with poor oral bioavailability due to the first pass metabolism. For improving the oral bioavailability, felodipine loaded solid lipid nanoparticles (SLNs) were developed using trimyristin, tripalmitin and glyceryl monostearate. Poloxamer 188 was used as surfactant. Lipid excipient compatibilities were confirmed by differential scanning calorimetry. SLN dispersions were prepared by hot homogenization of molten lipids and aqueous phase followed by ultrasonication at a temperature, above the melting point. SLNs were characterized for particle size, zeta potential, drug content, entrapment efficiency and crystallinity of lipid and drug. In vitro release studies were performed in 0.1N HCl and phosphate buffer of pH 6.8 using dialysis method. Pharmacokinetics of felodipine-SLNs after oral admini-stration in male Wistar rats was studied. The bioavailability of felodipine was increased by 1.75 fold when compared to that of a felodipine suspension.  

Development, in vitro and in vivo Evaluations of Solid-Lipid Microparticles based on Solidified Micellar Carrier System for Oral Delivery of Cefepime

2017 ◽  
Vol 10 (1) ◽  
pp. 3582-3593
Author(s):  
Chukwuebuka Umeyor ◽  
Uchechukwu Nnadozie ◽  
Anthony Attama
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Carrier System ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Release Study ◽  
Lipid Microparticles ◽  
Vitro Release

This study seeks to formulate and evaluate a solid lipid nanoparticle-based, solidified micellar carrier system for oral delivery of cefepime. Cefepime has enjoyed a lot of therapeutic usage in the treatment of susceptible bacterial infections; however, its use is limited due to its administration as an injection only with poor patient compliance. Since oral drug administration encourage high patient compliance with resultant effect in improved therapy, cefepime was formulated as solid lipid microparticles for oral delivery using the concept of solidified micellar carrier system. The carrier system was evaluated based on particle yield, particle size and morphology, encapsulation efficiency (EE %), and thermal analysis using differential scanning calorimeter (DSC). Preliminary microbiological studies were done using gram positive and negative bacteria. In vitro release study was performed using biorelevant media, while in vivo release study was performed in white albino rats. The yield of solid lipid microparticles (SLM) ranged from 84.2 – 98.0 %. The SLM were spherical with size ranges of 3.8 ± 1.2 to 42.0 ± 1.4 µm. The EE % calculated ranged from 83.6 – 94.8 %. Thermal analysis showed that SLM was less crystalline with high potential for drug entrapment. Microbial studies showed that cefepime retained its broad spectrum anti-bacterial activity. In vitro release showed sustained release of cefepime from SLM, and in vivo release study showed high concentration of cefepime released in the plasma of study rats. The study showed that smart engineering of solidified micellar carrier system could be used to improve oral delivery of cefepime.

Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

2013 ◽  
Vol 6 (4) ◽  
pp. 2269-2280
Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Release Formulation ◽  
Prokinetic Drug ◽  
Drug Entrapment Efficiency ◽  
Itopride Hydrochloride ◽  
Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

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