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.

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

scholarly journals FORMULATION AND EVALUATION OF DASATINIB LOADED SOLID LIPID NANOPARTICLES

2018 ◽  
Vol 10 (12) ◽  
pp. 14 ◽  
Author(s):  
M. Yasmin Begum ◽  
Prathyusha Reddy Gudipati
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Size Analysis ◽  
Compatibility Study ◽  
Solid Lipid ◽  
Poly Dispersity Index

Objective: The aim of present work was to formulate and evaluate Dasatinib (DST) loaded solid lipid nanoparticles (SLNs) as a potential anticancer drug delivery system by enhancing its solubility.Methods: SLNs consist of a solid lipid matrix where the drug was incorporated. Surfactants of GRAS grade were used to avoid aggregation and to stabilize the SLNs. DST-SLNs formulations of varying concentrations were prepared by high speed homogenization technique and evaluated for drug excipients compatibility study, poly-dispersity index, particle size analysis, surface morphology, zeta potential and drug release features.Results: It was observed that DST-SLNs with optimum quantities of poloxomer: lecithin ratio showed 88.06% drug release in 6h with good entrapment efficiency of 76.9±0.84 %. Particle size, Poly dispersity index, zeta potential and drug entrapment efficiency for the optimized formulation was found to be optimum. Stability studies revealed that the entrapment efficiency of the SLN dispersion stored in 4 °C was stable.Conclusion: Thus, it can be concluded that formulations of DST loaded SLNs are suitable carriers for improving the solubility and dissolution related problems. 

scholarly journals Atorvastatin Solid Lipid Nanoparticles as a Promising Approach for Dermal Delivery and an Anti-inflammatory Agent

2020 ◽  
Vol 21 (7) ◽  
Author(s):  
Seyed Sadegh Shahraeini ◽  
Jafar Akbari ◽  
Majid Saeedi ◽  
Katayoun Morteza-Semnani ◽  
Shidrokh Abootorabi ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Inflammatory Agent ◽  
Drug Entrapment Efficiency ◽  
Anti Inflammatory ◽  
Dermal Delivery

Abstract In the current research, the main focus was to overcome dermal delivery problems of atorvastatin. To this end, atorvastatin solid lipid nanoparticles (ATR-SLNs) were prepared by ultra-sonication technique. The prepared SLNs had a PDI value of ≤ 0.5, and the particle size of nanoparticles was in the range 71.07 ± 1.72 to 202.07 ± 8.40 nm. It was noticed that, when the concentration of lipid in ATR-SLNs increased, the size of nanoparticles and drug entrapment efficiency were also increased. Results showed that a reduction in the HLB of surfactants used in the preparation of SLN caused an increase in the particle size, zeta potential (better stability), and drug entrapment efficiency. Despite Tween and Span are non-ionic surfactants, SLNs containing these surfactants showed a negative zeta potential, and the absolute zeta potential increased when the concentration of Span 80 was at maximum. DSC thermograms, FTIR spectra, and x-ray diffraction (PXRD) pattern showed good incorporation of ATR in the nanoparticles without any chemical interaction. In vitro skin permeation results showed that SLN containing atorvastatin was capable of enhancing the dermal delivery of atorvastatin where a higher concentration of atorvastatin can be detected in skin layers. This is a hopeful promise which could be developed for clinical studies of the dermal delivery of atorvastatin nanoparticles as an anti-inflammatory agent.

scholarly journals Experimental Study on the Resistance of Synthetic Penicillin Solid Lipid Nanoparticles to Clinically Resistant Staphylococcus aureus

2021 ◽  
Vol 2021 ◽  
pp. 1-7
Author(s):  
Enliang Zhao ◽  
Tonghui Yi ◽  
Juan Du ◽  
Jing Wang ◽  
Shan Cong ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Lipid Nanoparticles ◽  
Inhibitory Effect ◽  
Polydispersity Index ◽  
Drug Resistant ◽  
Solid Lipid

Background. With the increasing resistance of antibiotics to bacteria, new and effective methods are needed to transform existing antibiotics to solve the problem of long development cycles for new drugs. The antibiotic nanodelivery system has proven to be a promising strategy. Aim. The purpose of this study is to synthesize penicillin solid lipid nanoparticles (penicillin SLNs) to enhance the antibacterial activity of penicillin against drug-resistant Staphylococcus aureus. Materials and Methods. Penicillin SLNs were synthesized. And particle size, the polydispersity index (PI), and zeta potential (ZP) of penicillin SLNs were measured. The surface morphology of penicillin SLNs was observed using a transmission electron microscope. Results. The particle size of penicillin SLNs is 112.3 ± 11.9   nm , the polydispersity index (PI) and zeta potential (ZP) of penicillin SLNs are 0.212 ± 0.03 and − 27.6 ± 5.5   mV . The encapsulation efficiency and drug loading were 98.31 ± 1.2 % and 4.98 ± 0.05 ( % w / w ), respectively. Penicillin SLNs had a more significant inhibitory effect on the growth of methicillin-sensitive Staphylococcus aureus (MSSA) after the drug and the bacteria were incubated for 12 hours. The number of MRSA colonies in the penicillin group increased after 12 hours, while the number of MRSA colonies in the penicillin SLNs group did not change significantly. Conclusion. Penicillin SLNs enhance the ability of penicillin to enter cells and increase the concentration of penicillin in the cell and also extend the residence time of penicillin in the cell. Our findings indicated that penicillin SLNs enhance the inhibitory effect of penicillin on drug-resistant Staphylococcus aureus.

scholarly journals Evaluation and Comparison of Solid Lipid Nanoparticles (SLNs) and Nanostructured Lipid Carriers (NLCs) as Vectors to Develop Hydrochlorothiazide Effective and Safe Pediatric Oral Liquid Formulations

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 437
Author(s):  
Paola Mura ◽  
Francesca Maestrelli ◽  
Mario D’Ambrosio ◽  
Cristina Luceri ◽  
Marzia Cirri
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Physical Stability ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Nanostructured Lipid Carriers ◽  
Particle Size Reduction ◽  
Solid Lipid ◽  
Oral Liquid

The aim of this study was the optimization of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in terms of physicochemical and biopharmaceutical properties, to develop effective and stable aqueous liquid formulations of hydrochlorothiazide, suitable for paediatric therapy, overcoming its low-solubility and poor-stability problems. Based on solubility studies, Precirol® ATO5 and Transcutol® HP were used as solid and liquid lipids, respectively. The effect of different surfactants, also in different combinations and at different amounts, on particle size, homogeneity and surface-charge of nanoparticles was carefully investigated. The best formulations were selected for drug loading, and evaluated also for entrapment efficiency and release behaviour. For both SLN and NLC series, the use of Gelucire® 44/14 as surfactant rather than PluronicF68 or Tween® 80 yielded a marked particle size reduction (95–75 nm compared to around 600–400 nm), and an improvement in entrapment efficiency and drug release rate. NLC showed a better performance than SLN, reaching about 90% entrapped drug (vs. 80%) and more than 90% drug released after 300 min (vs. about 65%). All selected formulations showed good physical stability during 6-month storage at 4 °C, but a higher loss of encapsulated drug was found for SLNs (15%) than for NLCs (<5%). Moreover, all selected formulations revealed the absence of any cytotoxic effect, as assessed by a cell-viability test on Caco-2 cells and are able to pass the intestinal epithelium as suggested by Caco-2 uptake experiments.

scholarly journals Hyaluronate Targeted Solid Lipid Nanoparticles of Etoposide: Optimization andIn VitroCharacterization

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Parviz Mohammadi Ghalaei ◽  
Farshid Hassanzadeh
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Aqueous Phase ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Cationic Lipid ◽  
Lipid Nanoparticles ◽  
Cetyl Alcohol ◽  
Phase Ratio ◽  
Solid Lipid

The aim of the present study was preparation of hyaluronan (HA) targeted solid lipid nanoparticles (SLNs) of etoposide. SLNs were prepared by an emulsification-solvent evaporation method and physically coated with HA. Four variables, including the ratio of cetyl alcohol to cationic lipid, cationic lipid type (stearylamine (SA) or dodecylamine (DDA)), lipid to HA ratio, and organic to aqueous phase ratio, were studied in an irregular fraction factorial design. Four responses, including particle size, zeta potential, drug loading, and 24-hour release efficiency percent, were measured for each formulation and then the optimization was carried out. The percent of HA coated on the SLNs was calculated by CHN elemental analysis which was shown to be about 55.89%. The cationic lipid type and the ratio of cetyl alcohol to cationic lipid had the highest influence on particle size and zeta potential, respectively. The highest effects of the ratio of lipid to HA and the organic to aqueous phase ratio were on the drug loading efficiency of SLNs. The optimized formulation of SLNs was obtained by SA, the equal proportion of cetyl alcohol and cationic lipid, the ratio of 1.5 for lipid to HA, and 10% of organic phase to aqueous phase.

Folate conjugated solid lipid nanoparticle: formulation development, optimization and characterization

2021 ◽  
Vol 11 ◽  
Author(s):  
Vaibhav Rajoriya ◽  
Varsha Kashaw ◽  
Sushil Kumar Kashaw
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
In Vitro Drug Release ◽  
Solid Lipid ◽  
Release Study

Objective: The current paper represents the development, optimization, and characterization of paclitaxel-loaded folate conjugated solid lipid nanoparticles (FA-SLNs). Methods: The ligand (FA-SLNs) conjugated and non-conjugated SLNs (PTX-SLNs) were prepared by hot homogenization method. Both of the formulations (FA-SLNs and PTX-SLNs) were optimized with various parameters i.e. drug loading, stirring time, stirring speed, particle size, and polydispersity index, and characterized. The in-vitro drug release study was performed in different pH environments by using the dialysis bag method. The surface morphology and particle size were determined through scanning electron micorscopy and Transmission Electron Microscopy respectively, The SLNs formulations were also evaluated for the stability study. Result: The particle size of PTX-SLNs and FA-SLNs was determined and found to be 190.1±1.9 and 231.3±2.3 nm respectively. The surface morphology of the SLNs indicates that the prepared formulations are round-shaped and show smooth surfaces. The TEM study indicated that particles were in the range of 100-300 nm. The entrapment efficiency and drug loading capacity of FA-SLNs were found to be 79.42±1.6% and 17.3±1.9%, respectively. In-vitro drug release study data, stated that the optimum drug release was found in an acidic environment at pH 4.0, that showed 94.21% drug release after 16 hours and it proves that optimized formulation FA-SLNs will gave the sustained and better release in tumor tissue that owing acidic environment because of the angiogenesis process. Conclusion: In this research paper, different formulation parameters, found to influence fabrication of drug into Solid lipid nanoparticles, were optimized for high entrapment efficiency and drug loading. The most important parameters were drug:lipid ratio, drug:polymer ratio and lipid: surfactant ratio. Higher in-vitro drug release was observed in pH 4 as compared to the pH 7.4. These result data concludes that FA-SLNs formulation was successfully prepared, optimized and characterized.

Research: Design, development and optimization of ramipril solid lipid nanoparticles using solvent emulsification and evaporation method

2019 ◽  
Vol 09 ◽  
Author(s):  
Rohan R. Vakhariya ◽  
Vijay R. Salunkhe ◽  
Dheeraj S. Randive ◽  
Mangesh A. Bhutkar ◽  
Somnath D. Bhinge
Keyword(s):  
Particle Size ◽  
Side Effects ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Evaporation Method ◽  
Solid Lipid ◽  
Particle Size Analyzer

Background: Ramipril, an antihypertensive drug exhibit 28% of oral bioavailability and also expelled quickly through the kidneys. Moreover, numerous side effects reported by the ramipril such as, hypotension (postural), increasing potassium level, and angioedema, when presented as an immediate dosage form. Hence, to conquer the side-effects associated with the drug and to increase its bioavailability. Objective: The intention of the proposed approach was to design, develop and optimize Ramipril loaded solid lipid nanoparticles. Methods: Solvent emulsification and evaporation method were employed to prepare Ramipril loaded solid lipid nanoparticles containign stearic acid and phosphatidylcholine as a lipid and surfactant respectively. The prepared formulations have been confirmed with particle size analyzer, %entrapment efficiency, Zeta Potential, SEM, X-ray diffraction study, FTIR, NMR spectroscopy, in-vitro release study and stability study. Result: The obtained results were noted to be within the standard limits. No interaction between Ramipril and other excipients, were confirmed with the FT-IR study of the formulations. Particle size analyzer confirmed that the nanometer size of prepared formulations ranges between 200-350nm. Percent entrapment efficiency was observed in the range of 70.61–91.60%. Entrapment and particle size results of the nanoparticles from R5 batch was an adjudged. The designed formulation noted 70.50% cumulative drug release within a period of 7hrs. The designed batch showed mean of zeta potential at-29.4 mV exhibiting good stability of formulation. Conclusion: The developed formulation was found to be stable and safe, and represents a promising system for the sustained and controlled delivery of Ramipril.

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 Development and Evaluation of Lapatinib Solid Lipid Nanoparticles in the Management of Breast Cancer

2019 ◽  
Vol 11 (05) ◽  
Author(s):  
Pamu Sandhya
Keyword(s):  
Breast Cancer ◽  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Drug Dissolution ◽  
Dissolution Studies ◽  
Solid Lipid

The current research was aimed at formulation of Lapatinib loaded solid lipid nanoparticles (SLNs) followed by evaluation for effective treatment of breast cancer. The formulations prepared by homogenization and ultrasonication and evaluated for zeta potential, particle size, polydispersity index, entrapment efficiency and in- vitro dissolution studies. Entrapment efficiency studies indicated proportional relation between concentration of lipid and the amount of drug entrapped. The physicochemical parameter evaluation data indicated 94.27% entrapment efficiency, 130 nm particle size and -19.9 zeta potential for stable formulation. The in vitro drug dissolution studies indicated that Lapatinib loaded SLNs (F6) formulated with Dynasan 116 and Egg Lecithin was suitable for anti-cancer therapy with higher drug dissolution rate.

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