Development and investigation of Artemether loaded binary solid lipid nanoparticles: Physicochemical characterization and in-situ single-pass intestinal permeability

2020 ◽  
Vol 60 ◽  
pp. 102072
Author(s):  
Anuj Garg ◽  
Devendra Singh Tomar ◽  
Kripal Bhalala ◽  
Muhammad Wahajuddin
2006 ◽  
Vol 6 (9) ◽  
pp. 2959-2966 ◽  
Author(s):  
Na Zhang ◽  
Qineng Ping ◽  
Guihua Huang ◽  
Xiuzhen Han ◽  
Yanna Cheng ◽  
...  

Wheat germ agglutinin (WGA) modified liposomes and solid lipid nanoparticles (SLNs) were evaluated for improving intestinal absorption of insulin. In an in situ local intestinal perfusion experiment, formulations containing 100 IU/kg insulin were administered to the duodenum, jejunum, and ileum of fasted rats. As hypothesized, ileum was the best intestinal location for the absorption of insulin-containing liposomes. Serum insulin concentrations decreased for the various formulations in different absorption sites according to the following trends: Duodenum > ileum > jejunum for WGA-modified insulin-containing liposomes; duodenum > jejunum > ileum for WGA-modified insulin-containing SLNs; ileum > jejunum > duodenum for insulin-containing liposomes; ileum > duodenum > jejunum for insulin-containing SLNs; and duodenum ≥ ileum > jejunum for aqueous solution of insulin. These results imply that the nanoparticle type and delivery site were important factors with respect to increasing the bioavailability of insulin following oral administration. The proteolytic degradation as well as the epithelial permeability were primary determinants influcing insulin mucosal absorption.


Author(s):  
Kobra Kohansal ◽  
Abdollah Rafiei ◽  
Heibatullah Kalantari ◽  
Ali Jelowdar ◽  
Anayatollah Salimi ◽  
...  

Purposes: Cystic echinococcosis (CE) is a serious contemporary public health problem. Different CE treatment methods are of considerable importance, with albendazole (ABZ) being one of the most preferred drugs for CE treatment and prophylaxis. In this study, we evaluated the nephrotoxicity caused by ABZ and ABZ-loaded solid lipid nanoparticles (SLNs) in mice with experimental hydatid cyst. Methods: ABZ-loaded SLNs were produced by micro-emulsification and a high shear homogenization technique. Thereafter, we evaluated the physicochemical characterization of the product. Live protoscolices were injected into mice to induce experimental hydatidosis. Mice were then treated with ABZ and ABZ-loaded SLNs. The nephrotoxicity effects were evaluated by biochemical and histopathological surveys. Results: Significantly different blood urea nitrogen (BUN) levels were observed between the two infected groups (ABZ treatment and ABZ-loaded SLN treatment) and the control group. The kidney malondialdehyde (MDA) and glutathione (GSH) levels of the infected groups were not significantly different from those of the control group. The histopathological study revealed nephropathic and pathologic changes in the ABZ and ABZ-loaded SLN groups. Conclusion: ABZ formulated for ABZ-loaded SLNs had a more prominent chemoprophylactic efficacy on CE and fewer side effects than ABZ alone. Neither ABZ nor ABZ-loaded SLNs caused significant biochemical and histopathological defects on the kidney, and all functional biochemical markers stayed within the normal range. Therefore, ABZ-loaded SLNs could be a potential new product for CE treatment.


Author(s):  
Jayachandra Reddy Peddappi Reddigari ◽  
Yerikala Ramesh ◽  
Chandrasekhar B. Kothapalli

The present research work “Formulation and Evaluation of In-situ gels enriched with Tropicamide loaded solid lipid nanoparticles”. To overcome the problems of side effects and to increase the bioavailability of tropicamide loaded solid lipid nanoparticles are containing with suitable lipids (glycerin trimyristate, Tristearin, Phosphatidylcholine & soyabean lecithin) with stabilizers (poloxamer 188) and surfactant like polysorbate 80. The interaction between drug, lipids & polymer by performing with FTIR no incompatibility with each other. The particle morphology was carried out by SEM & AFM in solid lipid nanoparticle formulation. The particle size was ranges from 213.6 ± 2.16nm to 538.0 ± 6.53 nm. The zeta potential ranges form -18.3mV to 25.6mV. The entrapment efficiency of free tropicamide was ranges from 74.13 % to 90.17%. The drug content was ranges from 0.212mg/ml to 0.912mg/ml. The SLN formulations must be transparent white colour and semi solid consistency. The pH 7.0 to 8.0 in all formulation. The gelling strength of gels TSLNGF1 to TSLNGF12 was ranges from 72 ± 1 sec to 117 ± 2 sec. The bio adhesive force was ranges from 10.12 ±1.01 dynes/cm2 to 23.12 ± 1.91 dynes/cm2. The viscosity of prepared formulation ranges from 415 ± 1.94 cps to 652 ± 1.41 cps. The spread ability studies of all formulation were ranges from 09 gms/sec to 18 gms/sec. The Accelerated stability the formulations does not undergo any chemical Changes. In vitro Franz’s diffusion studies of SLN enriched in gels TSLNGF1 to TSLNGF12 among the various formulation best formulations was TSLNGF6; its follows first order kinetics. Keywords: Solid Lipid Nanoparticles; Tropicamide; In- situ gels; In vitro diffusion studies


2021 ◽  
Author(s):  
Burcu Üner ◽  
Samet Özdemir ◽  
Çetin Taş ◽  
Yıldız Özsoy ◽  
Melike Üner

Abstract Purpose Loteprednol etabonate (LE) is a new generation corticosteroid that is used for the treatment of inflammatory and allergic conditions of the eye, and management of seasonal allergic rhinitis nasally. LE which is a poorly soluble drug with insufficient bioavailability, has a high binding affinity to steroid receptors. Sophisticated colloidal drug delivery systems of LE could present an alternative for treatment of inflammatory and allergic conditions of the skin. For this purpose, solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were attempted to improve for transdermal LE delivery for the first time. Methods SLN and NLC were produced by hot homogenization and ultrasonication technique. Formulations were characterized by dynamic light scattering, scanning electron microscopy, fourier transform infrared spectroscopy and differential scanning calorimetry. Their physical stability was monitored for 3 months of storage. Drug release profiles and permeation properties of SLN and NLC through the porcine skin were investigated. Results It was determined that SLN and NLC below 150 nm particle size had a homogeneous particle size distribution as well as high drug loading capacities. They were found to be stable both physically and chemically at room temperature for 90 days. In terms of release kinetics, it was determined that they released from SLN and NLC in accordance with Fickian diffusion release. Formulations prepared in this study were seen to significantly increase drug penetration through pig skin compared to the control group (p ≤ 0.05). Conclusion SLN and NLC formulations of LE can be stated among the systems that can be an alternative to conventional systems with less side-effect profile in the treatment of inflammatory problems on the skin.


Nanomaterials ◽  
2018 ◽  
Vol 9 (1) ◽  
pp. 33 ◽  
Author(s):  
Akshaya Tatke ◽  
Narendar Dudhipala ◽  
Karthik Janga ◽  
Sai Balguri ◽  
Bharathi Avula ◽  
...  

Triamcinolone acetonide (TA), an intermediate acting corticosteroid, is used in the treatment of posterior ocular diseases, such as inflammation, posterior uveitis, and diabetic macular edema. The objective of this investigation was to prepare TA-loaded solid lipid nanoparticles (TA-SLNs) and in situ gel (TA-SLN-IG) formulations for delivery into the deeper ocular tissues through the topical route. TA-SLNs were prepared by hot homogenization and ultrasonication method using glyceryl monostearate and Compritol® 888ATO as solid lipids and Tween®80 and Pluronic® F-68 as surfactants. TA-SLNs were optimized and converted to TA-SLN-IG by the inclusion of gellan gum and evaluated for their rheological properties. In vitro transcorneal permeability and in vivo ocular distribution of the TA-SLNs and TA-SLN-IG were studied using isolated rabbit corneas and New Zealand albino rabbits, respectively, and compared with TA suspension, used as control (TA-C). Particle size, PDI, zeta potential, assay, and entrapment efficiency of TA-SLNs were in the range of 200–350 nm, 0.3–0.45, −52.31 to −64.35 mV, 70–98%, and 97–99%, respectively. TA-SLN-IG with 0.3% gellan gum exhibited better rheological properties. The transcorneal permeability of TA-SLN and TA-SLN-IG was 10.2 and 9.3-folds higher compared to TA-C. TA-SLN-IG showed maximum tear concentration at 2 h, indicating an improved pre-corneal residence time, as well as higher concentrations in aqueous humor, vitreous humor and cornea at 6 h, suggesting sustained delivery of the drug into the anterior and posterior segment ocular tissues, when compared to TA-SLN and TA-C. The results, therefore, demonstrate that the lipid based nanoparticulate system combined with the in situ gelling agents can be a promising drug delivery platform for the deeper ocular tissues.


Cosmetics ◽  
2020 ◽  
Vol 7 (2) ◽  
pp. 42 ◽  
Author(s):  
Sandra Rubiano ◽  
Juan D. Echeverri ◽  
Constain H. Salamanca

The development and physicochemical characterization of solid lipid nanoparticles (SLNs) with potential for formulating hair cosmetic products were carried out. SLNs were made from Otoba wax, which is native to the tropical Andean region and has a high chemical composition of fatty acids with intermediate chains. SLNs were formulated by preparing wax-in-water dispersions at two internal phase proportions (low = 5% w/w and high = 20% w/w), using the same ratio of surfactant system and preservatives. The coarse dispersions were subjected to ultrahigh pressure homogenization (UHPH), and thermal stability assays for 4 weeks were carried out, where changes in Creaming Index, droplet size, polydispersity, viscosity, zeta potential, conductivity, and pH were evaluated. The results showed that Otoba wax has a required HLB value around 9 and is mainly composed of lauric (~35%) and myristic (~45%), which have been reported to improve the condition of hair loss. Regarding the development on SLNs, it was found that the internal phase concentration did not considerably affect the physicochemical and microbiological properties. Likewise, it was found that UHPH enabled the production of SLNs with particle sizes <200 nm, low polydispersity (<0.3), high zeta potential values, and suitable physical and microbiological stability. Therefore, Otoba wax has potential for the development of SLNs applicable to cosmetic formulations, especially for hair products.


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