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.

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

Solid lipid nanoparticle loaded with paromomycin: in vivo efficacy against Leishmania tropica infection in BALB/c mice model

2016 ◽  
Vol 100 (16) ◽  
pp. 7051-7060 ◽  
Author(s):  
Maryam Heidari-Kharaji ◽  
Tahereh Taheri ◽  
Delaram Doroud ◽  
Sima Habibzadeh ◽  
Sima Rafati
Keyword(s):  
Leishmania Tropica ◽  
Solid Lipid Nanoparticle ◽  
Mice Model ◽  
In Vivo Efficacy ◽  
Solid Lipid ◽  
Lipid Nanoparticle

Sustained release of piroxicam from solid lipid nanoparticle as an effective anti-inflammatory therapeutics in vivo

2016 ◽  
Vol 43 (1) ◽  
pp. 55-66 ◽  
Author(s):  
Li-Hua Peng ◽  
Wei Wei ◽  
Ying-Hui Shan ◽  
Yee-Song Chong ◽  
Lian Yu ◽  
...  
Keyword(s):  
Sustained Release ◽  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Lipid Nanoparticle ◽  
Anti Inflammatory

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 Design, Synthesis, Anticancer Activity, and Solid Lipid Nanoparticle Formulation of Indole- and Benzimidazole-Based Compounds as Pro-Apoptotic Agents Targeting Bcl-2 Protein

2021 ◽  
Vol 14 (2) ◽  
pp. 113
Author(s):  
Manar I. Nagy ◽  
Khaled M. Darwish ◽  
Safaa M. Kishk ◽  
Mohamed A. Tantawy ◽  
Ali M. Nasr ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticle ◽  
Rt Pcr ◽  
Design Synthesis ◽  
Structural Modifications ◽  
Solid Lipid ◽  
Lipid Nanoparticle ◽  
Anti Cancer ◽  
Nanoparticle Formulation ◽  
New Compounds

Cancer is a multifactorial disease necessitating identification of novel targets for its treatment. Inhibition of Bcl-2 for triggered pro-apoptotic signaling is considered a promising strategy for cancer treatment. Within the current work, we aimed to design and synthesize a new series of benzimidazole- and indole-based derivatives as inhibitors of Bcl-2 protein. The market pan-Bcl-2 inhibitor, obatoclax, was the lead framework compound for adopted structural modifications. The obatoclax’s pyrrolylmethine linker was replaced with straight alkylamine or carboxyhydrazine methylene linkers providing the new compounds. This strategy permitted improved structural flexibility of synthesized compounds adopting favored maneuvers for better fitting at the Bcl-2 major hydrophobic pocket. Anti-cancer activity of the synthesized compounds was further investigated through MTT-cytotoxic assay, cell cycle analysis, RT-PCR, ELISA and DNA fragmentation. Cytotoxic results showed compounds 8a, 8b and 8c with promising cytotoxicity against MDA-MB-231/breast cancer cells (IC50 = 12.69 ± 0.84 to 12.83 ± 3.50 µM), while 8a and 8c depicted noticeable activities against A549/lung adenocarcinoma cells (IC50 = 23.05 ± 1.45 and 11.63 ± 2.57 µM, respectively). The signaling Bcl-2 inhibition pathway was confirmed by molecular docking where significant docking energies and interactions with key Bcl-2 pocket residues were depicted. Moreover, the top active compound, 8b, showed significant upregulated expression levels of pro-apoptotic/anti-apoptotic of genes; Bax, Bcl-2, caspase-3, -8, and -9 through RT-PCR assay. Improving the compound’s pharmaceutical profile was undertaken by introducing 8b within drug-solid/lipid nanoparticle formulation prepared by hot melting homogenization technique and evaluated for encapsulation efficiency, particle size, and zeta potential. Significant improvement was seen at the compound’s cytotoxic activity. In conclusion, 8b is introduced as a promising anti-cancer lead candidate that worth future fine-tuned lead optimization and development studies while exploring its potentiality through in-vivo preclinical investigation.

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