Effect of Surfactant on Characteristics of Solid Lipid Nanoparticles (SLN)

2011 ◽  
Vol 364 ◽  
pp. 313-316 ◽  
Author(s):  
Karn Orachai Kullavadee ◽  
Ruktanonchai Uracha ◽  
Siwaporn Meejoo Smith
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Drug Carrier ◽  
Tween 80 ◽  
Lipid Nanoparticles ◽  
Great Promise ◽  
Solid Lipid ◽  
Alternative Drug ◽  
Model Drug ◽  
Drug Free

SLN have shown a great promise as an alternative drug carrier for intravenous and dermal applications. This work focuses on the basic properties of drug-free Compritol® ATO 888 based SLN systems by using cationic surfactant (CPC) and nonionic surfactant (Tween 80). Effects of surfactant on the physical properties of SLNs were investigated in the absence of model drug to avoid the interaction between drug and surfactant. These SLN samples have different particle size, zeta potential and morphology. DSC was used to quantify the crystallinity of SLN systems. It was found that %RI of both SLNs was similar, indicating that types of surfactant did not affect on crystallization of solid lipid. Spherical-like particle was observed with SLN-C, while rod-like particle was found with SLN-T. The results demonstrated that surfactant plays an important role on SLN physical characteristics.

scholarly journals PREPARATION, CHARACTERIZATION, AND FORMULATION OF SOLID LIPID NANOPARTICLES LOTION FROM MULBERRY ROOTS (MORUS ALBA L.)

2020 ◽  
pp. 182-186
Author(s):  
MUHAMAD WILDAN NUGRAHA ◽  
RADITYA ISWANDANA ◽  
MAHDI JUFRI
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
High Speed ◽  
Tween 80 ◽  
Lipid Nanoparticles ◽  
Morus Alba ◽  
Glyceryl Monostearate ◽  
Optimum Result ◽  
Solid Lipid

Objective: Tween 80 has been used as a solvent for the extraction of phenolic compounds because this surfactant has both hydrophilic and hydrophobicproperties. Solid lipid nanoparticles (SLNs) have been developed to improve penetration through the skin layer. We investigated the efficacy of usingthe microwave-assisted micellar extraction (MAME) approach for extracting oxyresveratrol from Morus alba roots and also to develop an SLN lotion.Methods: The M. alba roots were extracted with Tween 80 in a microwave for 18 min, and the extract was used to develop SLN with differentconcentrations of glyceryl monostearate. The SLNs from M. alba root extracts were prepared by a high-speed homogenization technique (25,000 rpmfor 15 min). The SLNs produced were characterized as per particle size, polydispersity index (PDI), and zeta potential. The SLNs with the bestcharacteristics were used to formulate a lotion using a high-pressure homogenizer.Results: Extraction using MAME showed improved extraction efficiency. The oxyresveratrol concentration from the extract was 2.77%. The SLN with2.5% glyceryl monostearate showed the optimum result, with a particle size of 130.20 nm, a PDI of 0.278, and a zeta potential of −21.8 mV. The SLNlotion exhibited a particle size of 285.9 nm and a PDI of 0.360. The SLN lotion also had good penetration, with a flux of 4.70 μg cm−2/h.Conclusion: MAME is an efficient method for extracting oxyresveratrol from M. alba roots. The SLN with 2.5% glyceryl monostearate exhibited theoptimum characteristics, and the SLN lotion showed good characteristics, including skin penetration.

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.

scholarly journals Formulation and Evaluation of Solid Lipid Nanoparticles of Olanzapine for the Treatment of Psychosis

2020 ◽  
Vol 10 (5-s) ◽  
pp. 25-31
Author(s):  
Shubhangi C. Daswadkar ◽  
Abhijit Vasant Atole
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
High Speed ◽  
Entrapment Efficiency ◽  
Antipsychotic Agent ◽  
Tween 80 ◽  
Lipid Nanoparticles ◽  
Particle Size Analysis ◽  
Size Analysis ◽  
Solid Lipid

Solid lipid nanoparticles (SLN) are typically spherical with an average diameter between 1 nm to 1000 nm in range. It is alternative carrier systems to tradition colloidal carriers, such as liposomes emulsions and polymeric micro and nanoparticles. Olanzapine (OZP) is an atypical antipsychotic agent which is used for treatment of Schizophrenia. Its oral bioavailability is around of 40%. OZP is a class II drug so it having low aqueous solubility. To overcome that problem and to increase its bioavailability, the solid lipid nanoparticles of olanzapine are prepared. Formulation batches designed by modifying type of surfactant ( Span 80, Tween 80), concentration of surfactant, Concentration of co-surfactant, type of lipid ( glyceryl monostearate, Stearic acid), Lipid concentration, speed of stirring and time of stirring using customised design  of DOE. The SLN were prepared by high speed homogenization technique, and then characterized by particle size analysis, Drug entrapment efficiency and Drug diffusion study. A formulation containing GMS as a lipid stabilised with tween 80 as surfactant show good drug release, smaller particle size, as compared with other formulations with different lipid and surfactant. The present research findings indicate that OZP loaded solid lipid Nano particulate system for delivery of OZP with better efficacy with minimum adverse effects. Keywords: Olanzapine, SLN, GMS, high speed homogenization and DOE.

Preparation, Characterization and In-vitro release of Piroxicam-loaded Solid Lipid Nanoparticles

2010 ◽  
Vol 3 (3) ◽  
pp. 1136-1146
Author(s):  
V K Verma ◽  
Ram A
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Diffusion Method ◽  
Solid Lipid ◽  
Vitro Release

 Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h. 

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

Optimization of Solid Lipid Nanoparticles of Ezetimibe in Combination with Simvastatin Using Quality by Design (QbD)

2020 ◽  
Vol 10 (4) ◽  
pp. 404-418
Author(s):  
Kruti Borderwala ◽  
Ganesh Swain ◽  
Namrata Mange ◽  
Jaimini Gandhi ◽  
Manisha Lalan ◽  
...  
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
High Speed ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Water Soluble ◽  
Lipid Matrix ◽  
Solid Lipid ◽  
32 Factorial Design ◽  
Full Factorial Experimental Design

Background: The objective of this study was to develop solid lipid nanoparticles (SLNs) of poorly water soluble anti-hyperlipidemic drugs-Ezetimibe in combination with Simvastatin. Methods: This study describes a 32 full factorial experimental design to optimize the formulation of drug loaded lipid nanoparticles (SLN) by the high speed homogenization technique. The independent variables amount of lipid (GMS) and amount of surfactant (Poloxamer 188) were studied at three levels and arranged in a 32 factorial design to study the influence on the response variables- particle size, % entrapment efficiency (%EE) and cumulative drug release (% CDR) at 24 h. Results: The particle size, % EE and % CDR at 24 h for the 9 batches (B1 to B9) showed a wide variation of 104.6-496.6 nm, 47.80-82.05% (Simvastatin); 48.60-84.23% (Ezetimibe) and 54.64-92.27% (Simvastatin); 43.8-97.1% (Ezetimibe), respectively. The responses of the design were analysed using Design Expert 10.0.2. (Stat-Ease, Inc, USA), and the analytical tools of software were used to draw response surface plots. From the statistical analysis of data, polynomial equations were generated. Optimized formulation showed particle size of 169.5 nm, % EE of 75.43% (Simvastatin); 79.10% (Ezetimibe) and 74.13% (Simvastatin); 77.11% (Ezetimibe) %CDR after 24 h. Thermal analysis of prepared solid lipid nanoparticles gave indication of solubilisation of drugs within lipid matrix. Conclusion: Fourier Transformation Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating no interaction between drugs and lipid matrix and being only dissolved in it. Electron microscope of transmission techniques indicated sphere form of prepared solid lipid nanoparticles with smooth surface with size approximately around 100 nm.

scholarly journals Development of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers of Loteprednol Etabonate: Physicochemical Characterization and Ex Vivo Permeation Studies

2021 ◽  
Author(s):  
Burcu Üner ◽  
Samet Özdemir ◽  
Çetin Taş ◽  
Yıldız Özsoy ◽  
Melike Üner
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Physicochemical Characterization ◽  
Lipid Nanoparticles ◽  
Nanostructured Lipid Carriers ◽  
Fickian Diffusion ◽  
Control Group ◽  
Loteprednol Etabonate ◽  
Solid Lipid

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.

scholarly journals Enhancement of ciprofloxacin activity by incorporating it in solid lipid nanoparticles

2020 ◽  
Vol 19 (5) ◽  
pp. 909-918
Author(s):  
Saqer Alarifi ◽  
Salam Massadeh ◽  
Mohammed Al-Agamy ◽  
Manal A.l. Aamery ◽  
Abdulkareem Al Bekairy ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Release Profile ◽  
Drug Release Profile ◽  
Solid Lipid

Purpose: To incorporate ciprofloxacin (CIP) into solid lipid nanoparticles (SLN) in order to enhance its biopharmaceutical properties and antibacterial activity.Methods: A sonication melt-emulsification method was employed for the preparation of CIP-loaded SLN. The composition of the SLN was varied in order to investigate factors such as lipid type and combination ratio, drug to lipid ratio, and surfactant ratio. The produced SLN formulations wereevaluated for their particle size and shape, zeta potential, and entrapment efficiency. In addition, the effect of SLN formulation composition on its drug release profile and antimicrobial activity against Escherichia coli, Pseudomonas Aeruginosa, and Staphylococcus Aureus was also investigated.Results: The generated nanoparticles had particle size in the range of 165 to 320 nm. The zetapotential values were generally low within ± 5. All formulations exhibited entrapment efficiency between 50 and 90 %. CIP release exhibited a biphasic release profile with a low burst phase, followed by uniform controlled-release behavior of various rates. SLN-loaded CIP exhibited one-fold reduction in minimum inhibitory concentration (MIC) and caused significant inhibition of all the three bacterial strains tested, when compared with pure CIP.Conclusion: Loading of CIP into SLN significantly enhances its antimicrobial activity in vitro which can translate to significant enhancement of therapeutic outcomes by minimizing the dose-dependent adverse and side effects and/or enhancing the antimicrobial spectrum of activity. Keywords: Solid lipid nanoparticles, Sonication melt-emulsification, Ciprofloxacin, Escherichia coli, Pseudomonas aeruginosa

Development of Mupirocin- Tinidazole solid- Lipid Nanoparticles Loaded Topical gel for the Management of Bacterial Wound Infections

2021 ◽  
pp. 2785-2790
Author(s):  
Veintramuthusankar Veintramuthusankar ◽  
Pushparajudayakumar Pushparajudayakumar ◽  
Rajanduraibabyroselin Rajanduraibabyroselin
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Fickian Diffusion ◽  
Standard Drug ◽  
Topical Gel ◽  
Solid Lipid ◽  
Homogenization Technique ◽  
Significant Difference

Solid lipid nanoparticles (SLNs) are novel drug carrier system which consists of a solid matrix composed of a lipid being solid at both room and body temperatures with a mean Particle Size (PS) between 50 and 1000 nm Mupirocin -Tinidazole solid-lipid nanoparticles were prepared using hot homogenization technique using Glyceryl monosterate, Stearic acid, Tween 80 and Poloxamer 188 using hot homogenization technique. Size of the nanoparticles was in the range of 83 to 211 nm with the zeta potential values between -2.1 to -5.2. Atomic Force Microscopy (AFM) confirms the spherical shape of solid lipid nanoparticles. Entrapment efficiency was best in the F1 formulation. In vitro release of the pure drug was found to be 75% of mupirocin and 66.5% of tinidazole at the end of 1 hr. Drug release from SLNs dispersion followed Korsermeyrs peppas-model, indicating fickian diffusion drug release, while that from the gel followed non Fickian model drug release. Antibacterial activity of the SLNs was less but the SLNs based gel shows no significant difference in activity to that of standard drug gentamycin against aerobic bacteria. The SLNs dispersion exhibited physicochemical stability under refrigeration upto 45 days without significant difference in particle size. Best formulation was developed into a topical gel using sodium alginate and it was evaluated for pH, viscosity, spreadbility, extrudability, bloom strength, Minimum Inhibitory Concentration (MIC) and Methicillin resistant staphylococcus aureus (MRSA). Extrudability and spreadability parameters of the gel are similar to that of marketed Mupirocin 2% cream formulation

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