Zeta Potential Of Solid Lipid Nanoparticles Research Articles

Fabrication of Transdermal Gel Embedded with Solid Lipid Nanoparticles of Indomethacin

Rheumatoid/osteoarthritis is one of the most common causes for lacking behind in the health sector. Medication in the form of tablets are already available in the market but has disadvantages. When these medicines are taken orally it cause heartburn and discomfort. The introduction of transdermal drug delivery is expected to solve this problem of side eff ects associated with oral delivery of drug. In the present study, indomethacin was loaded in solid lipid nanoparticles (SLN) which are then embedded in Carbopol gel for transdermal application. The solvent evaporation ultrasonication method was used for making SLNs. The formulation was evaluated for various parameters such as ; particle size and zeta potential of SLN using zetasizer as an instrument and gel formulations were evaluated for pH, spreading coeffi cient, viscosity, visual appearance and clarity. Gel-embedded SLN formulation was found to be a potential transdermal drug delivery system for NSAIDs like indomethacin to treat ailments like rheumatoid arthritis or osteoarthritis.

Practicality Assessment of a Frugal Nanoparticle Generator: Opening Doors to Nano Pharmaceuticals for the Researchers and Students of Underprivileged Academic Institutions

Background: Probe sonication and High-speed homogenizer are comparatively costly equipment to fabricate the nanoparticles. Many academic and research institutions cannot afford the procurement and maintenance of such sophisticated equipment. In the present work, a newer idea is conceptualized, which can be adopted by the underprivileged research institutions to fabricate solid lipid nanoparticles (SLN) in the absence of sophisticated equipment. The current work describes the pilot-level trials of this novel approach. This study represents the preliminary proof-of-concept trials for which the Indian patent application (3508/MUM/2015) is filed. Method: A frugal piece of equipment was made using a 50 ml centrifuge tube with conical bottom and a piezoelectric mist maker or humidifier. SLNs were prepared by combining the quasi-emulsion solvent evaporation approach and ultrasonic vibration approach. A quasi-emulsion was composed by the dropwise mixing of the organic solvent containing drug & lipid with an aqueous solution containing surfactant under continuous ultrasonic vibration in the piezoelectric chamber. The size of the droplets was significantly reduced due to piezoelectric ultrasonic vibration. Under the provision of mild vacuum and heat generated by vibration, the organic solvent was evaporated, which leaves behind a suspension of SLN. In the present work, albendazole was selected as a model drug. Various trials with Compritol 888 ATO® and Precirol ATO 5® as a lipid carrier and Tween 80 and Poloxamer 188 as a surfactant were performed. Zeta potential of SLNs was improved by the addition of polyelectrolytes like K2SO4 and Na4P2O7. Result and Conclusion: The ratio of drug to lipid was optimized to 1:4 for the most favorable results. SLN with a minimum Z-average diameter of 98.59 nm, -21 mV zeta potential, and 34.064 % (SD 10.78, n=9) entrapment efficiency were developed using the Precirol ATO 5 ® as a lipid carrier. The proof of concept for this novel approach is established through the development of Albendazole SLNs. This approach must also be evaluated for the development of polymeric nanoparticles and vesicular formulations. The further sophistication of the frugal equipment may allow more control over the quality of SLN. This approach will enable underprivileged researchers to prepare Nanopharmaceuticals. Researchers and students of such institutions can focus on the application of SLN by resolving the constraint of sophisticated equipment with this novel approach. This novel approach should also be tried for polymeric and vesicular nanopharmaceuticals.

Optimization of process variables of zanamivir-loaded solid lipid nanoparticles and the prediction of their cellular transport in Caco-2 cell model

The aim of this study was to optimize the process variables of zanamivir-loaded solid lipid nanoparticles (SLNs) and to predict their cellular transport across Caco-2 cell monolayers. Zanamivir-loaded SLNs were prepared by a double emulsion solvent evaporation method. The effects of process variables on the mean particle size and zeta potential of SLNs were investigated and the physicochemical properties of SLNs were characterized. In addition, the cytotoxicity and transport ability of SLNs were also studied in Caco-2 cell model. The mean particle size of drug-loaded SLNs was significantly affected by the process variables. The SLNs were prepared using glyceryl monosterate (1% polyvinyl alcohol (PVA) or 1.5% poloxamer 188 as surfactant) had a regular shape with a relatively lower mean particle size (324.2 and 224.9nm, respectively), higher encapsulation efficacy (55.7 and 42.4%, respectively) and sustained drug release over 12h. The crystalline form of drug had been partly changed and no physicochemical interaction had occurred between drug and carriers in SLNs. The cell viability was approximately 100% even at a high concentration of blank SLNs. There was no remarkable difference in drug permeation between drug-loaded SLNs and drug solution at 2h, while drug-loaded SLNs showed a significant decrease in drug permeation compared with the drug solution at 4h. The process variables of zanamivir-loaded SLNs were successfully optimized in this study. However, these SLNs significantly reduced the transport ability of zanamivir across Caco-2 cell monolayers. Further studies are needed to fully understand the real absorption mechanism of developed SLNs.

Effect of Solid Lipid Nanoparticles Formulation Compositions on Their Size, Zeta Potential and Potential for In Vitro pHIS-HIV-Hugag Transfection

This work was conducted to determine model equations describing the effect of solid lipid nanoparticles (SLN) formulation compositions on their size and zeta potential using the face-centered central composite design and to determine the effect of SLN formulation compositions on the potential for in vitro pHIS-HIV-hugag transfection. SLN were prepared by the hot high pressure homogenization technique using cetylpalmitate as lipid matrix at varying concentrations of Tween 80 and Span 85 mixture, dimethyldioctadecyl ammonium bromide (DDAB) and cholesterol. Size and zeta potential used as responses of the design were measured at pH 7.0. The model equations were accepted as statistical significance at p value of less than 0.05. Ability of SLN to form complex with pHIS-HIV-hugag was evaluated by electrophoretic mobility shift assay. In vitro cytotoxicity of SLN was studied in HeLa cells using alamar blue bioassay. The potential of SLN for in vitro pHIS-HIV-hugag transfection was also determined in HeLa cells by western blot technique. SLN possessed diameter in a range of 136-191 nm and zeta potential 11-61 mV depending on the concentrations of surfactant mixture, DDAB and cholesterol. The regression analysis showed that the model equations of responses fitted well with quadratic equations. The ability of SLN to form complex with pHIS-HIV-hugag was also affected by formulation compositions. In vitro cytotoxicity results demonstrated that HeLa cells were not well tolerant of high concentrations of SLN but still survived in a range of 100-200 microg/ml of SLN in culture medium. The results of transfection study showed ability of SLN to use as a vector for in vitro pHIS-HIV-hugag transfection. However, their potential for in vitro transfection was lower than the established transfection reagent. Size and zeta potential of SLN could be predicted from their quadratic model equations achieved by combination of three variables surfactant, DDAB and cholesterol concentrations. In addition, these variables also affected the potential of SLN as a vector for in vitro pHIS-HIV-hugag transfection. The results here provide the framework for further study involving the SLN formulation design for DNA delivery.

Pharmacokinetics, tissue distribution and bioavailability of nitrendipine solid lipid nanoparticles after intravenous and intraduodenal administration

Purpose: The aim of this research was to study whether the bioavailability of nitrendipine (NDP) could be improved by administering nitrendipine solid lipid nanoparticles (SLN) duodenally to rats.Methods: Nitrendipine was incorporated into SLN prepared by hot homogenization followed by ultrasonication method. SLN were produced using various triglycerides (trimyristin, tripalmitin and tristearin), soy phosphatidylcholine 95%, poloxamer 188 and charge modifiers (dicetyl phosphate, DCP and stearylamine, SA). Particle size and charge measurements were made with a Malvern Zetasizer. Pharmacokinetics of nitrendipine SLNs (NDP-SLNs) after intravenous (i.v.) and intraduodenal (i.d.) administration to conscious male Wistar rats were studied. Tissue distribution studies of NDP-SLNs were carried out in Swiss albino mice after i.v. administration and compared to nitrendipine suspension (NDP-Susp).Results: Average size and zeta potential of SLNs of different lipids, with and without charge modifiers ranged from 101.9 ± 3.0 to 123.5 ± 3.0 nm and − 35.1 ± 0.5 to +34.6 ± 2.3 mV, respectively. AUC(0–∞) was increased (up to 4.51-folds) and clearance was decreased (up to 4.54-folds) after i.v. administration of NDP-SLNs with and without charge modifiers compared to NDP-Susp. Effective bioavailability of NDP-SLNs were 2.81–5.35-folds greater after i.d. administration in comparison with that of NDP-Susp. In tested organs, the AUC and MRT of NDP-SLNs were higher than those of NDP-Susp especially in brain, heart and reticuloendothelial cells containing organs.Conclusions: SLN are suitable drug delivery systems for the improvement of bioavailability of nitrendipine. Negatively and positively charged SLN were better taken up by the liver and brain, respectively.

Preparation and characterization of solid lipid nanoparticles containing peptide

Solid lipid nanoparticles (SLN) are an alternative colloidal carrier system for controlled drug delivery. However, only a few have been studied regarding the incorporation of peptides into SLN, due to the hydrophilic peptide not easy to enter the lipophilic matrix of SLN. In the present report, peptide-loaded solid lipid nanoparticles were prepared by a novel solvent diffusion method in an aqueous system. The model peptide gonadorelin was incorporated to study the entrapment efficiency, size, zeta potential (charge) and drug delivery characterization. Gonadorelin and monostearin were dissolved in acetone and ethanol at 50 °C in water bath, the resultant organic solution was poured into an aqueous containing 1% polyvinyl alcohol (PVA) under mechanical agitation. The peptide-loaded solid lipid nanoparticles were quickly produced and separated by centrifugation. The average volume diameter of gonadorelin-loaded SLN is 421.7 nm and the zeta potential of SLN is −21.1 mV dispersed in distilled water. Up to 69.4% of gonadorelin can be incorporated. In vitro release of gonadorelin from SLN is slow. In the test solution of a 0.1N hydrochloric acid for 2 h and then transferred in a pH 6.8 phosphate buffer (simulative gastrointestinal fluid), the drug-release behavior from SLN suspension exhibited a biphasic pattern. After burst drug-release at the first 6 h at a percentage of 24.4% of loaded gonadorelin, a distinctly prolonged release over a monitored period of 12 days was observed and nearly 3.81% of drug was released in each day. In the test solution of a pH 6.8 phosphate buffer (simulative intestinal fluid), the drug-release rate from SLN was similar to that in the simulative gastrointestinal fluid. Further, a novel preparation method in the present research for peptide-loaded SLN was established. These results also demonstrate the principle suitability of SLN as a prolonged release formulation for hydrophilic peptide drugs.

Formulation parameters determining the physicochemical characteristics of solid lipid nanoparticles loaded with all-trans retinoic acid.

Solid lipid nanoparticles (SLNs) have gained attention as a colloidal drug carrier, particularly for drugs with limited solubility. The poor aqueous solubility of all-trans retinoic acid (ATRA) has been a limiting factor in its clinical use. This study was undertaken to overcome the solubility limitation of ATRA by loading in SLNs. The physicochemical characteristics of ATRA-loaded SLNs were investigated by particle size analysis, zeta potential measurement, thermal analysis and HPLC determination of ATRA content. The mean particle size of ATRA-loaded SLNs could be reduced (1) by mixing EggPC and Tween 80 as a surfactant and (2) by increasing the total surfactant amount. The smallest mean particle size of SLNs was obtained with 50 mg/g surfactant mixture composed of 54:46% (w/w) EggPC:Tween 80 (154.9 nm). The zeta potential of SLNs could be increased by mixing EggPC, Tween 80 and DSPE-PEG in the surfactant mixture. The zeta potential of SLNs prepared with 50 mg/g surfactant mixture composed of 48:6:46% (w/w) of EggPC:DSPE-PEG:Tween 80 was -38.18 mV. ATRA could be loaded at 2.4% (percentage of lipid matrix) on these SLNs without impairing their physical stability. After freeze-drying, the mean particle size and polydispersity index of ATRA-loaded SLNs were only slightly increased (181.8 vs. 265.2 nm, 0.173 vs. 0.200). Furthermore, no significant change was observed in the SLN-loaded concentration of ATRA and the zeta potential of SLNs after freeze-drying. Taken together, SLN formulation of ATRA with similar characteristics to those of parenteral emulsions could be obtained even after freeze-drying.