scholarly journals Intestinal Lymphatic Delivery of Praziquantel by Solid Lipid Nanoparticles: Formulation Design,In VitroandIn VivoStudies

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Amit Mishra ◽  
Parameswara Rao Vuddanda ◽  
Sanjay Singh
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Spherical Shape ◽  
Fold Increase ◽  
Storage Conditions ◽  
Lipid Nanoparticles ◽  
Homogeneous Distribution ◽  
Burst Release ◽  
Solid Lipid ◽  
Aqueous Surfactants ◽  
Lymphatic Delivery

The aim of the present work was to design and develop Praziquantal (PZQ) loaded solid lipid nanoparticles (PZQ-SLN) to improve the oral bioavailability by targeting intestinal lymphatic system. PZQ is practically insoluble in water and exhibits extensive hepatic first-pass metabolism. PZQ SLN were composed of triglycerides, lecithin and various aqueous surfactants; were optimized using hot homogenization followed by ultrasonication method. The optimized SLN had particle size of123±3.41 nm, EE of86.6±5.72%. The drug release of PZQ-SLN showed initial burst release followed by the sustained release. Inspite of zeta potential being around −10 mV, the optimized SLN were stable at storage conditions (5±3°C and25±2°C/60±5% RH) for six months. TEM study confirmed the almost spherical shape similar to the control formulations. Solid state characterization using differential scanning calorimeter (DSC) and powder X-ray diffraction (PXRD) analysis confirmed the homogeneous distribution of PZQ within the lipid matrix. The 5.81-fold increase inAUC0→∞, after intraduodenal administration of PZQ-SLN in rats treated with saline in comparison to rats treated with cycloheximide (a blocker of intestinal lymphatic pathway), confirmed its intestinal lymphatic delivery. The experimental results indicate that SLN may offer a promising strategy for improving the therapeutic efficacy and reducing the dose.

scholarly journals Preparation, characterization and scale-up of sesamol loaded solid lipid nanoparticles

2012 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Vandita Kakkar ◽  
Indu Pal Kaur
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Scale Up ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Transmission Electron ◽  
The Brain

Sesamol loaded solid lipid nanoparticles (SSLNs) were prepared with the aim of minimizing its distribution to tissues and achieving its targeting to the brain. Three scale-up batches (100x1 L) of S-SLNs were prepared using a microemulsification technique and all parameters were statistically compared with the small batch (1x;10 mL). S-SLNs with a particle size of less than 106 nm with a spherical shape (transmission electron microscopy) were successfully prepared with a total drug content and entrapment efficiency of 94.26±2.71% and 72.57±5.20%, respectively. Differential scanning calorimetry and infrared spectroscopy confirmed the formation of lipidic nanoparticles while powder X-ray diffraction revealed their amorphous profile. S-SLNs were found to be stable for three months at 5±3°C in accordance with International Conference on Harmonisation guidelines. The SLN preparation process was successfully scaled-up to a 100x batch on a laboratory scale. The procedure was easy to perform and allowed reproducible SLN dispersions to be obtained.

scholarly journals Preparation and Characterization of Solid Lipid Nanoparticles Loaded with Cisplatin

2018 ◽  
Vol 8 (6) ◽  
pp. 125-131
Author(s):  
Indrayani D. Raut ◽  
Rajendra C. Doijad ◽  
Shrinivas K. Mohite ◽  
Arehalli S. Manjappa
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Acquired Resistance ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Platinum Drug ◽  
Solid Lipid

Cisplatin (Cis diaminedichloro platinum) was the first platinum drug to be used as an anticancer drug, and it is widely used in the treatment of testicular, head, neck, ovarian and lung cancer. The use of Cisplatin is limited due to its intrinsic and acquired resistance and severe side effects such as chronic neurotoxicity and nephrotoxicity. The colloidal carriers such as emulsion, liposomes, polymeric nanoparticles have been extensively studied to overcome above limitations. The solid lipid nanoparticles (SLNs), amongst other colloidal carriers, were found to be an ideal carrier for lipophillic drug for better stability and release retardation. Cisplatin loaded solid lipid nanoparticles was prepared by microemulsion technique. Stearic acid was used as lipid. The other excipients were used as DPPG, Soya lecithin and Poloxamer P407  and acidic buffer  PH4. Also used Probe sonication for 10 min at 79 Amplitude. Cisplatin SLNs Batch C13 showed particle size of 119.23±1.52 nm, Zeta potential of -37.33±2.47 mV, % Entrapment efficiency of  90.2 ± 2.1 %., % Drug loading capacity of 1.62 ± 1.34 %., The TEM study of optimized Cisplatin SLN illustrated the spherical shape of nanoparticles. Total release amount of Cisplatin was 82.62± 2.04 % after 48 hrs. The formulation performed kinetics study followed Peppas plot equation The SLNs of Cisplatin met all the requirements of a colloidal drug delivery system. They had particle size in nanosize; their size distribution was narrow and all the particles were in spherical shape and stable. Keywords: Cisplatin, Solid Lipid nanoparticles, zeta potential, Particle size, Transmission electron Microscopy.

scholarly journals Central Composite Design for Formulation and Optimization of Solid Lipid Nanoparticles to Enhance Oral Bioavailability of Acyclovir

Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5432
Author(s):  
Haniza Hassan ◽  
Siti Khadijah Adam ◽  
Ekram Alias ◽  
Meor Mohd Redzuan Meor Mohd Affandi ◽  
Ahmad Fuad Shamsuddin ◽  
...  
Keyword(s):  
Central Composite Design ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Oral Drug Delivery ◽  
Entrapment Efficiency ◽  
Fold Increase ◽  
Lipid Nanoparticles ◽  
Oral Drug ◽  
Solid Lipid ◽  
Central Composite

Treatment of herpes simplex infection requires high and frequent doses of oral acyclovir to attain its maximum therapeutic effect. The current therapeutic regimen of acyclovir is known to cause unwarranted dose-related adverse effects, including acute kidney injury. For this reason, a suitable delivery system for acyclovir was developed to improve the pharmacokinetic limitations and ultimately administer the drug at a lower dose and/or less frequently. In this study, solid lipid nanoparticles were designed to improve the oral bioavailability of acyclovir. The central composite design was applied to investigate the influence of the materials on the physicochemical properties of the solid lipid nanoparticles, and the optimized formulation was further characterized. Solid lipid nanoparticles formulated from Compritol 888 ATO resulted in a particle size of 108.67 ± 1.03 nm with an entrapment efficiency of 91.05 ± 0.75%. The analyses showed that the optimum combination of surfactant and solid lipid produced solid lipid nanoparticles of good quality with controlled release property and was stable at refrigerated and room temperature for at least 3 months. A five-fold increase in oral bioavailability of acyclovir-loaded solid lipid nanoparticles was observed in rats compared to commercial acyclovir suspension. This study has presented promising results that solid lipid nanoparticles could potentially be used as an oral drug delivery vehicle for acyclovir due to their excellent properties.

scholarly journals Development and Characterization of Solid Lipid Nanoparticles Containing Herbal Extract: In Vivo Antidepressant Activity

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
P. Vijayanand ◽  
V. Jyothi ◽  
N. Aditya ◽  
A. Mounika
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Spherical Shape ◽  
Antidepressant Activity ◽  
Lipid Nanoparticles ◽  
Herbal Extract ◽  
Solid Lipid ◽  
Hibiscus Rosa Sinensis ◽  
Native Crude

In alternate systems of medicine like Ayurveda and traditional Chinese medicine, Hibiscus rosa sinensis and its extracts have been traditionally prescribed for their antidepressant activity. Crude extracts and rudimentary formulations approaches are good for proof-of-concept studies; however, these formulations are fraught with problems like poor oral bioavailability and high variability between subjects. Systematic drug delivery approaches could prove effective in addressing some of these problems. In this study, we report the development of Hibiscus rosa sinensis extract loaded solid lipid nanoparticles (HSLNs) using glycerol monostearate or beeswax as lipids. The HSLNs were evaluated for their size, surface charge, and morphology. The optimized HSLNs were tested for antidepressant activity in male Swiss albino mice. It was found that, with the optimized procedure, HSLNs of ~175 nm, carrying negative charge and nearly spherical shape, could be obtained. The in vivo test results suggested that there were marked differences in the immobility times of the test animals. Moreover, with HSLNs, it was found that at doses several times lower than the native crude extract dose, similar pharmacological effect could be obtained. These initial findings suggest that encapsulating phytopharmaceuticals into advanced delivery systems like solid lipid nanoparticles can be an effective strategy in improving their in vivo performance.

scholarly journals Evaluation of Conditions Affecting Properties of Gac (Momordica Cocochinensis Spreng) Oil-Loaded Solid Lipid Nanoparticles (SLNs) Synthesized Using High-Speed Homogenization Process

Processes ◽  
2019 ◽  
Vol 7 (2) ◽  
pp. 90 ◽  
Author(s):  
Huynh Mai ◽  
Thai Nguyen ◽  
Thi Le ◽  
Duy Nguyen ◽  
Long Bach
Keyword(s):  
Solid Lipid Nanoparticles ◽  
High Speed ◽  
Lipid A ◽  
Storage Temperature ◽  
Tween 80 ◽  
Storage Conditions ◽  
Lipid Nanoparticles ◽  
Homogenization Method ◽  
Solid Lipid ◽  
The Impact

In this study, we attempted the preparation of gac oil-loaded solid lipid nanoparticles (SLNs) by the high-speed homogenization method using Naterol SE solid lipid, a cosmetic self-emulsifying base, and surfactant and investigated the effects of different conditions on the characteristics of the resulting nanoparticles. The suspensions containing 5% active agents (gac-oil, w/w) were dispersed in a surfactant concentration of 5% (w/w) (Span 80:Tween 80 ratio of 28:72 w/w) and 2.5% (w/w) of solid lipid (Naterol SE) concentration. Suitable conditions for hot homogenization were 13,000 rpm, 60 min and 60 °C for speed, time and temperature, respectively. The suitable conditions for the subsequent cold homogenization were 25 min of homogenization time and 5 °C of temperature. The results showed that the mean size of SLNs-gac oil was 107 nm (measured by laser diffraction spectrometry, LDS), and dried size of SLNs-gac oil ranged from 50 to 80 nm (measured by transmission electron microscope, TEM). In addition, the study investigated the impact of gac oil content on the particle size of SLNs-gac oil and its stability under different storage conditions of UV radiation and storage temperature. At high storage temperatures, the color changes (ΔE) of the samples were more profound in comparison to that at the low storage temperature. The ΔE value of the blank sample (SLN-FREE gac-oil) was higher than that of the Gac oil-loaded SLNs samples (SLN-gac oil).

scholarly journals Lyophilized Drug-Loaded Solid Lipid Nanoparticles Formulated with Beeswax and Theobroma Oil

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 908
Author(s):  
Hilda Amekyeh ◽  
Nashiru Billa
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Colloidal Stability ◽  
Fold Increase ◽  
Active Pharmaceutical Ingredient ◽  
Lipid Nanoparticles ◽  
Systemic Availability ◽  
Solid Lipid ◽  
And Storage ◽  
Higuchi Model

Solid lipid nanoparticles (SLNs) have the potential to enhance the systemic availability of an active pharmaceutical ingredient (API) or reduce its toxicity through uptake of the SLNs from the gastrointestinal tract or controlled release of the API, respectively. In both aspects, the responses of the lipid matrix to external challenges is crucial. Here, we evaluate the effects of lyophilization on key responses of 1:1 beeswax–theobroma oil matrix SLNs using three model drugs: amphotericin B (AMB), paracetamol (PAR), and sulfasalazine (SSZ). Fresh SLNs were stable with sizes ranging between 206.5–236.9 nm. Lyophilization and storage for 24 months (4–8 °C) caused a 1.6- and 1.5-fold increase in size, respectively, in all three SLNs. Zeta potential was >60 mV in fresh, stored, and lyophilized SLNs, indicating good colloidal stability. Drug release was not significantly affected by lyophilization up to 8 h. Drug release percentages at end time were 11.8 ± 0.4, 65.9 ± 0.04, and 31.4 ± 1.95% from fresh AMB-SLNs, PAR-SLNs, and SSZ-SLNs, respectively, and 11.4 ± 0.4, 76.04 ± 0.21, and 31.6 ± 0.33% from lyophilized SLNs, respectively. Thus, rate of release is dependent on API solubility (AMB < SSZ < PAR). Drug release from each matrix followed the Higuchi model and was not affected by lyophilization. The above SLNs show potential for use in delivering hydrophilic and lipophilic drugs.

scholarly journals Preparation and characterization of topical solid lipid nanoparticles containing deferoxamine

2021 ◽  
Vol 62 (3) ◽  
pp. 224-234
Author(s):  
Masoud Ali Karami ◽  
Behzad Sharif Makhmalzadeh ◽  
Narges Mosaddegh Rad
Keyword(s):  
Differential Scanning Calorimetry ◽  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Burst Release ◽  
Scanning Calorimetry ◽  
Diabetic Ulcer ◽  
Solid Lipid

Introduction: Deferoxamine mesylate increases hypoxia inducible factor-1 alpha transactivation by preventing iron-catalyzed reactive oxygen stress, so it can be used to improve diabetic ulcer healing. This study was undertaken to develop and study physicochemical properties of topical deferoxamine-loaded solid lipid nanoparticles. Method: Solid lipid nanoparticles were prepared using cold homogenization technique and full factorial design to evaluate the effect of surfactant type and amount of lipid. In-vitro characterization of formulations including particle size and distribution, thermal behavior using Differential Scanning Calorimetry, entrapment efficiency, and release profile were carried out. Results: The results showed an acceptable range of particle size (2.88–174 nm), a narrow size distribution, and an average of 60% for drug entrapment efficiency which is significant for a hydrophilic drug. The results from release study showed an initial burst release followed by a slow and prolonged manner. Differential Scanning Calorimetry results also confirmed the results obtained from loading and release evaluations. The best formulation which had a high level of drug loading and the lowest drug release rate contained compritol and oleic acid in the amount of 8% of the total formula, as well as tween 80 and lecithin as a mixture of surfactants. Conclusions: The study demonstrated deferoxamine could be loaded in solid lipid nanoparticles to deliver topically.

scholarly journals DESIGN, DEVELOPMENT AND CHARACTERIZATION OF PACLITAXEL LOADED SOLID LIPID NANOPARTICLES AS A COLLOIDAL DRUG CARRIER

2019 ◽  
pp. 333-340
Author(s):  
INDRAYANI D. RAUT ◽  
AREHALLI S. MANJAPPA ◽  
SHRINIVAS K. MOHITE ◽  
RAJENDRA C. DOIJAD
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Stearic Acid ◽  
Solid Lipid Nanoparticles ◽  
Drug Carrier ◽  
Drug Loading ◽  
Spherical Shape ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Soya Lecithin

Objective: This study was aimed to design and characterize Paclitaxel-loaded Solid Lipid Nanoparticles (SLNs) to achieve site specificity,reduce toxicity and sustained release pattern. Methods: Paclitaxel-loaded solid lipid nanoparticles were fabricated by microemulsion followed by probe sonication technique using stearic acid as lipid and stabilized of the mixture of surfactants. In this study, 32 full factorial design was employed for optimizing the concentration of lipid as stearic acid and surfactant (soya lecithin) for the nanoparticles. The optimization was done by studying the dependent variable of particle size and % entrapment efficiency. Results: The results showed that the paclitaxel-loaded solid lipid nanoparticles prepared with the concentration of 33.31 % stearic acid and 500 mg of soya lecithin were optimum characteristic than other formulations. They showed the average particles size 149±4.10 nm and PDI 250±2.04. The zeta potential, % EE and % drug loading capacity was found to be respectively-29.7, 93.38±1.90 and 0.81±0.01. The optimized batch of Paclitaxel SLNs exhibited spherical shape with smooth surface analyzed by Transmission Electron Microscopy. In vitro study showed sustained release profile and was found to follow Higuchi Kinetics Equation. Conclusion: The SLNs of paclitaxel m et al. l the requirements of a colloidal drug delivery system. They had a particle size in nanosize; their size distribution was narrow and all the particles were in a spherical shape.

Solid Lipid Nanoparticles and Chitosan-coated Solid Lipid Nanoparticles as Promising Tool for Silybin Delivery: Formulation, Characterization, and In vitro Evaluation

2018 ◽  
Vol 16 (2) ◽  
pp. 142-152 ◽  
Author(s):  
Vieri Piazzini ◽  
Lorenzo Cinci ◽  
Mario D'Ambrosio ◽  
Cristina Luceri ◽  
Anna Rita Bilia ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Solid Lipid Nanoparticles ◽  
Cell Monolayer ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Water Soluble ◽  
Burst Release ◽  
Solid Lipid ◽  
Vitro Release

Background: Silybin (Sb) is the major flavolignan of the extract of Silybum marianum. It is used for the treatment of various acute and chronic liver toxicities, inflammation, fibrosis and oxidative stress. Many studies indicate that Sb is also active against different carcinomas and it has been very recently proposed to be beneficial in type 2 diabetes patients. However, Sb is a low water soluble and low permeable compound. Objective: In this study, Solid Lipid Nanoparticles (SLNs) were proposed to enhance the solubility and the intestinal absorption of Sb. </P><P> Methods: SLNs were made of stearic acid and Brij 78 and subsequently coated with chitosan. Formulations were physically and chemically characterized. Stability studies were also assessed. Sb in vitro release was evaluated in different pH media. In vitro permeability test with artificial membranes and Caco-2 cells were performed. Cellular uptake and mucoadhesion studies were conducted. Results: Both nanoparticles were found to be stable. In vitro release indicated that SLNs may prevent burst release and gastric degradation of Sb. Higher extent of Sb permeation was observed for both nanoparticles in PAMPA and Caco-2 cell monolayer models. The results of the cellular uptake study suggested the involvement of active endocytic processes. Chitosan significantly improves mucoadhesion properties of nanoparticles. </P><P> Conclusions: Together with the excellent stability, strong mucoadhesive property, and slow release, chitosan coated SLNs demonstrated promising potential to enhance absorption of hydrophobic Sb after oral administration.

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