scholarly journals USING A SIMPLEX CENTROID DESIGN AND FATTY ACIDS TO OPTIMIZE FLUCONAZOLE-LOADED SOLID LIPID NANOPARTICLES (SLNs)

2021 ◽  
pp. 206-209
Author(s):  
PAKORN KRAISIT ◽  
NAMON HIRUN ◽  
PREMJIT LIMPAMANOCH ◽  
SONTAYA LIMMATVAPIRAT
Keyword(s):  
Fatty Acids ◽  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Weak Acid ◽  
Polydispersity Index ◽  
Solid Lipid ◽  
Predicted Values ◽  
Experimental Values

Objective: This study aimed to prepare fluconazole (FZ)-loaded solid lipid nanoparticles (SLNs) using a simplex centroid design and fatty acids to optimize the SLNs to get small-sized nanoparticles with a narrow distribution. Methods: Hot emulsification was used to prepare the FZ-loaded SLNs. Stearic acid (Sa) (X1), palmitic acid (Pa) (X2), and myristic acid (Ma) (X3) were the solid lipids. The effect of various types and amounts of fatty acids on the particle size, polydispersity index, zeta potential, and pH of the SLNs was studied using the simplex centroid design. Results: The particle size of all formulations ranged between 16.49 nm and 56.65 nm, and the polydispersity index (PDI) ranged between 0.258 and 0.676, indicating a relatively narrow size distribution. The zeta potential ranged from–7.47 to–12.2 mV. The pH was around 4.63–4.77, indicating that the SLN system was a weak acid. Design-Expert® software was used to design the responses of all model formulations and to select the optimized formulation. The optimal formulation comprised 0.190 g Sa, 0.048 g Pa, and 0.002 g Ma. The experimental values of the particle size and PDI of the optimal formulation did not differ significantly from the predicted values and lay within a 95% confidence interval (CI). Conclusion: Therefore, the simplex centroid design using fatty acids could efficiently formulate and optimize FZ-loaded SLNs.

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 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 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 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.

Formulation and Evaluation of Solid Lipid Nanoparticles for controlled delivery of Zidovudine

2021 ◽  
pp. 2548-2556
Author(s):  
Sonia Dhiman ◽  
Gurjeet Singh Thakur ◽  
Shivangi Anand ◽  
Priyanka Yadav
Keyword(s):  
Drug Delivery ◽  
High Pressure ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Controlled Drug Delivery ◽  
Lipid Nanoparticles ◽  
Polydispersity Index ◽  
High Pressure Homogenization ◽  
X Ray ◽  
Solid Lipid

Zidovudine is one of the chief nucleoside analogue and reverse inhibitor licensed for HIV infection which is placed along with a group of retroviruses. The present research study on Zidovudine solid dosage form surveyed the feasibility utilizing solid lipid nanoparticles (SLNs) for controlled drug delivery of zidovudine embracing glyceryl behenate as lipidic material, tween 80 as a stabilizer and blend of sodium chelate with poloxamer as surfactant. The SLNs were prepared utilizing high pressure homogenization followed by ultrasonication method. The prepared SLNs were characterized by particle size analysis, polydispersity index, zeta potential, DSC, TEM, IR spectroscopy, and X-ray diffractometry. Narrow size distribution of the particles was marked having polydispersity index values under 0.8. The high zeta potential of the different SLN formulations additionally showed their physical stability. Differential scanning calorimetry and powder X-ray diffraction showed decline in crystallinity of drug in the nanoparticle formulation. In vitro release study showed sustained release for up to 12 hours in the SLN formulations prepared. The current study results revealed that zidovudine SLN formulation prepared by high pressure homogenization followed by ultrasonication is a suitable method for controlled drug delivery system.

scholarly journals PREPARATION OF SOLID LIPID NANOPARTICLES CONTAINING MANGOSTEEN PERICARP EXTRACT

2018 ◽  
Vol 11 (15) ◽  
pp. 80
Author(s):  
Siti Nur Diniyanti
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Physical Characteristics ◽  
Protection Factor ◽  
Potential Value ◽  
Solid Lipid ◽  
Sun Protection Factor ◽  
Viscous Substance

Objectives: The aim of this study was to develop solid lipid nanoparticles (SLNs) containing mangosteen pericarp extract (MPE) to achieve enhanced photoprotection and to provide an alternative to synthetic sunscreens in the market.Materials and Methods: The MPE was prepared using the maceration method, and evaluated for sun protection factor (SPF) value using an ultraviolet (UV)-Vis spectrophotometer. SLNs were prepared through ultrasonication method. Blank-SLNs were formulated using stearic acid (SA) or palmitic acid (PA) as solid lipids at a concentration of 3%. Tween® 80 or polyvinyl alcohol (PVA) was employed as a surfactant with a concentration ranging from 1 to 2%. The obtained blank-SLNs were investigated for their physical characteristics, (i.e., morphology, particle size, polydispersity index [PDI], and zeta potential values). The blank-SLNs with suitable physical characteristics were selected to encapsulate MPE and evaluated for the physical characteristics.Results: The MPE was a brownish viscous substance with an SPF value that ranged from 3.09±0.005 to 27.20±0.05 at a concentration ranging from 0.02 to 0.1 mg/ml. Based on the physical characteristics, the blank-SLNs employing PA or SA with 1% of PVA were selected. The MPE-SLNs were spherical, with a particle size that ranged from 443.51±6.50 to 533.52±16.15 nm; PDI ranged from 0.35±0.008 to 0.459±0.02, and zeta potential value ranged from 18.32±1.37 to −19.03±0.64. The entrapment efficiencies of MPE-PA-SLNs and MPE-SA-SLNs were 83.24±1.37% and 84.17±0.411%, respectively.Conclusion: The results indicated the promising potential of MPE as a UVB photoprotector. The MPE-SLNs were also successfully formulated, but, further study is needed to confirm the potential of MPE-SLNs to be used as a sunscreen, and their stability during storage.

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.

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 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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