scholarly journals Selection of Cryoprotectant in Lyophilization of Progesterone-Loaded Stearic Acid Solid Lipid Nanoparticles

Pharmaceutics ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 892 ◽  
Author(s):  
Timothy M. Amis ◽  
Jwala Renukuntla ◽  
Pradeep Kumar Bolla ◽  
Bradley A. Clark
Keyword(s):  
Particle Size ◽  
Stearic Acid ◽  
Solid Lipid Nanoparticles ◽  
High Speed ◽  
Sodium Taurocholate ◽  
Polarized Light ◽  
Lipid Nanoparticles ◽  
Stability Study ◽  
Solid Lipid ◽  
Selection Of

Cryoprotectants are often required in lyophilization to reduce or eliminate agglomeration of solute or suspended materials. The aim of this study was to select a cryoprotecting agent and optimize its concentration in a solid lipid nanoparticle formulation. Progesterone-loaded stearic acid solid lipid nanoparticles (SA-P SLNs) were prepared by hot homogenization with high speed mixing and sonication. The stearic acid content was 4.6% w/w and progesterone was 0.46% w/w of the initial formulation. Multiple surfactants were evaluated, and a lecithin and sodium taurocholate system was chosen. Three concentrations of surfactant were then evaluated, and a concentration of 2% w/w was chosen based on particle size, polydispersity, and zeta potential. Agglomeration of SA-P SLNs after lyophilization was observed as measured by increased particle size. Dextran, glycine, mannitol, polyvinylpyrrolidone (PVP), sorbitol, and trehalose were evaluated as cryoprotectants by both an initial freeze–thaw analysis and after lyophilization. Once selected as the cryoprotectant, trehalose was evaluated at 5%, 10%, 15%, and 20% for optimal concentration, with 20% trehalose being finally selected as the level of choice. Evaluation by DSC confirmed intimate interaction between stearic acid and progesterone in the SA-P SLNs, and polarized light microscopy shows successful lyophilization of the trehalose/SA-P SLN. A short term 28-day stability study suggests the need for refrigeration of the final lyophilized SA-P SLNs in moisture vapor impermeable packaging.

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 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.

Optimizing the Size of Drug-Loaded Nanoparticles Using Design of Experiments

2020 ◽  
pp. 131-157
Author(s):  
Paola Cervantes-Covarrubias ◽  
Ayla Vea-Barragan ◽  
Aracely Serrano-Medina ◽  
Eugenia Gabriela Carrillo-Cedillo ◽  
José Manuel Cornejo-Bravo
Keyword(s):  
Particle Size ◽  
Design Of Experiments ◽  
Design Of Experiment ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Fractional Factorial ◽  
Solid Lipid ◽  
Two Factors ◽  
Nanoparticle System ◽  
Selection Of

Nanoparticles formed from lipids are currently applied successfully to deliver drugs. The particle size of the nanoparticle system is an essential characteristic to enhance the entrance of the drugs inside tissues and cells. Using design of experiment is appealing to find the specific conditions to optimize particle size of drug-loaded nanoparticles. Authors of this chapter applied a fractional factorial design of half fraction 24-1 with levels between continue factors, finding statistically significant differences for two factors such as concentrations of drugs and type of solvent where the organic phase is dissolved. This design shows the optimization of a formulation of capsaicin in solid lipid nanoparticles. The chapter also includes information on methods to prepare solid lipid nanoparticles (SLN), the variables involved, and a selection of studies about optimization of SLN formulations.

scholarly journals REVIEW ARTIKEL: SOLID LIPID NANOPARTICLES (SLN) METODE DAN KARAKTERISTIK

2020 ◽  
Vol 3 (2) ◽  
pp. 307-316
Author(s):  
Ilhanni Khoerunisa ◽  
◽  
Aji Najihudin ◽  
Siti Hindun
Keyword(s):  
Particle Size ◽  
Small Particle ◽  
Solid Lipid Nanoparticles ◽  
High Speed ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Absorption Efficiency ◽  
Small Particle Size ◽  
Solid Fat ◽  
Solid Lipid

Solid Lipid Nanoparticles are composed of active substances, solid fats, water and surfactants. SLN has advantages by having a small particle size of 50-1000 nm and a large absorption efficiency value of 40-100%. SLN has a homogeneous particle size with a IP value that is closed to zero. One of the methods used to produce SLN is HSH/ High pressure homogeneity where the process uses pressure to produce small particle size. The HSH/ High-speed homogeneity method uses stirring speed as a parameter in the manufacture of nanoparticles. Solvent emulsification method does not use high temperatures in the homogeneity process. The most important SLN characteristics are particle size and entrapment efficiency values. These characteristics are strongly influenced by large concentration of solid fat and surfactants. The greater amount of the surfactant used, the smaller the particle size and the increasing value of the trap efficiency. If the solid fat concentration used is greater, the particle size will be as larger, but the absorption efficiency value will be greater because the fat will provide more space for the active substance to be entrapped.

Optimizing the Size of Drug-Loaded Nanoparticles Using Design of Experiments

2021 ◽  
pp. 330-356
Author(s):  
Paola Cervantes-Covarrubias ◽  
Ayla Vea-Barragan ◽  
Aracely Serrano-Medina ◽  
Eugenia Gabriela Carrillo-Cedillo ◽  
José Manuel Cornejo-Bravo
Keyword(s):  
Particle Size ◽  
Design Of Experiments ◽  
Design Of Experiment ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Fractional Factorial ◽  
Solid Lipid ◽  
Two Factors ◽  
Nanoparticle System ◽  
Selection Of

Nanoparticles formed from lipids are currently applied successfully to deliver drugs. The particle size of the nanoparticle system is an essential characteristic to enhance the entrance of the drugs inside tissues and cells. Using design of experiment is appealing to find the specific conditions to optimize particle size of drug-loaded nanoparticles. Authors of this chapter applied a fractional factorial design of half fraction 24-1 with levels between continue factors, finding statistically significant differences for two factors such as concentrations of drugs and type of solvent where the organic phase is dissolved. This design shows the optimization of a formulation of capsaicin in solid lipid nanoparticles. The chapter also includes information on methods to prepare solid lipid nanoparticles (SLN), the variables involved, and a selection of studies about optimization of SLN formulations.

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

Solid lipid nanoparticles of stearic acid for the drug delivery of paliperidone

RSC Advances ◽  
2015 ◽  
Vol 5 (84) ◽  
pp. 68743-68750 ◽  
Author(s):  
Sacheen Kumar ◽  
Jaspreet Kaur Randhawa
Keyword(s):  
Drug Delivery ◽  
Stearic Acid ◽  
Antipsychotic Drug ◽  
Solid Lipid Nanoparticles ◽  
Water Solubility ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Poor Water Solubility

Paliperidone is an antipsychotic drug having poor water solubility and bioavailability. Solid lipid nanoparticles of stearic acid loaded with paliperidone were prepared to enhance the bioavailability.

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