scholarly journals Design and Evaluation of Voriconazole Loaded Solid Lipid Nanoparticles for Ophthalmic Application

2016 ◽  
Vol 2016 ◽  
pp. 1-11 ◽  
Author(s):  
Anubha Khare ◽  
Inderbir Singh ◽  
Pravin Pawar ◽  
Kanchan Grover

Voriconazole is a second-generation antifungal agent with excellent broad spectrum of antifungal activity commercially available for oral and intravenous administration. Systemic administration of voriconazole is associated with side effects including visual and hepatic abnormalities. This study assessed the feasibility of using solid lipid nanoparticles for ocular delivery of voriconazole adopting stearic acid as lipidic material, tween 80 as a stabilizer, and Carbopol 934 as controlled release agent and for increasing the precorneal residence time in eye. The systems were prepared using two different methods, that is, ultrasonication method and microemulsion technique. The results indicated that the larger particle size of SLNs was found with microemulsion technique (308±3.52 nm to 343±3.51) compared to SLN prepared with ultrasonication method (234±3.52 nm to 288±4.58 nm). The polydispersity index values were less than 0.3 for all formulations and zeta potential of the prepared formulations by these two methods varied from −22.71±0.63 mV to −28.86±0.58 mV. Powder X-ray diffraction and differential scanning calorimetry indicated decrease in crystallinity of drug. The in vitro release study and the SLN formulations prepared with ultrasonication method demonstrated sustained release up to 12 hours. This study demonstrated that SLN prepared by ultrasonication method is more suitable than microemulsion technique without causing any significant effect on corneal hydration level.

2012 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Vandita Kakkar ◽  
Indu Pal Kaur

Sesamol loaded solid lipid nanoparticles (SSLNs) were prepared with the aim of minimizing its distribution to tissues and achieving its targeting to the brain. Three scale-up batches (100x1 L) of S-SLNs were prepared using a microemulsification technique and all parameters were statistically compared with the small batch (1x;10 mL). S-SLNs with a particle size of less than 106 nm with a spherical shape (transmission electron microscopy) were successfully prepared with a total drug content and entrapment efficiency of 94.26±2.71% and 72.57±5.20%, respectively. Differential scanning calorimetry and infrared spectroscopy confirmed the formation of lipidic nanoparticles while powder X-ray diffraction revealed their amorphous profile. S-SLNs were found to be stable for three months at 5±3°C in accordance with International Conference on Harmonisation guidelines. The SLN preparation process was successfully scaled-up to a 100x batch on a laboratory scale. The procedure was easy to perform and allowed reproducible SLN dispersions to be obtained.


Author(s):  
AMRUTHA U ◽  
SUSHMITHA B ◽  
SHAIK RUBINA ◽  
PADMINI IRIVENTI

Objective: The objective of the present study was to formulate and evaluate caffeine loaded solid lipid nanoparticles (SLNs) in the treatment of clinical mastitis. Methodology: These were prepared by homogenization technique using cholesterol, tween 80, and chloroform as excipients. Preformulation studies such as ultraviolet spectrophotometry, Fourier transform infrared (FTIR), and differential scanning calorimetry (DSC) were performed for the drug. Entrapment efficiency and in vitro dissolution studies were carried out for prepared SLN’s and the optimum formulation (F2) was taken for further studies such as FTIR, DSC, scanning electron microscopy, particle size, and zeta potential analysis. Results: Obtained results stated that prepared SLNs are roughly spherical in nature and are in nanorange. These were incorporated in Carbopol gel and further evaluation studies such as pH, spreadability, viscosity, homogeneity, and in vitro drug diffusion studies were carried out. All the results obtained state that prepared nanogel has shown sustained release of drug. The antimicrobial study was carried out using Staphylococcus aureus and it was confirmed by appearance of the zone of inhibition. Conclusion: Nanogel that contains Caffeine SLNs with 1:2 ratio drug:lipid has shown good in vitro release. Sustained release of Caffeine drug till 12 h was achieved by delivering it in the form of nanogel.


Author(s):  
Botre P.P ◽  
Maniyar M.G.

The objective of this study was to develop suitable solid lipid nanoparticles for topical delivery of Bifonazole. Bifonazole is an imidazole antifungal drug used in form of ointments. It was patented in 1974 and approved for medical use in 1983. Bifonazole having broad spectrum activity against dermatophytes, moulds, yeasts, fungi and some gram positive bacteria. BFZ SLNs systems were developed by melt emulsification followed by solvent evaporation technique using Compritol 888ATO (Glyceryl behenate) as a solid lipid and Tween 80 as a surfactant. Developed SLNs were evaluated for particle size, polydispersity index (PI), entrapment efficiency (EE) and drug release profiles. Process and formulation parameters were optimized. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) studies were carried out on SLNs to mark the changes in the drug and lipid modifications. The BFZ SLNs based gels were prepared using Carbopol 940 as a gelling agent. The SLNs based gels were evaluated for rheological parameters, in vitro drug release and permeation studies. In vitro antifungal study suggested that the SLNs based gel was more effective in inhibiting growth of Candida albicans. Thus the study concludes that SLNs based gel of BFZ gives a sustained release profile of BFZ and has the potential for treatment of topical fungal infections.


2011 ◽  
Vol 108 (1) ◽  
pp. 191-196 ◽  
Author(s):  
Ellen Denise P. Almeida ◽  
Adjane A. Costa ◽  
Mairim R. Serafini ◽  
Fábia C. Rossetti ◽  
Juliana M. Marchetti ◽  
...  

2020 ◽  
Vol 11 (11) ◽  
pp. 685-700
Author(s):  
Omar Sarheed ◽  
Douha Shouqair ◽  
KVRNS Ramesh ◽  
Muhammad Amin ◽  
Joshua Boateng ◽  
...  

Aim: To prepare loratadine-loaded solid lipid nanoparticles (SLNs) using a modified two-step ultrasound-assisted phase inversion temperature (PIT) process. Results/methodology: Loratadine was dissolved in beeswax and Tween 80 was dissolved in water. The two phases were mixed together to prepare a water-in-oil emulsion preconcentrate (w/o) at a PIT of 85°C, followed by gradual water addition at 25°C to trigger nanoparticles formation (o/w). Kinetic stability was investigated. No change in the size was observed within 6 months. Fourier-transform infrared spectroscopy demonstrated stability of the emulsions via molecular structure of water at the interface of the o/w nanoemulsions. SLNs enhanced the in vitro skin permeation of loratadine. Conclusion: Stable SLNs were successfully prepared by ultrasound-assisted PIT.


2012 ◽  
Vol 62 (4) ◽  
pp. 547-562 ◽  
Author(s):  
Golmohammadzadeh Shiva ◽  
Mortezania Somaye ◽  
Jaafari Mahmoud Reza

The aim of this study was to develop new solid lipid nanoparticles of isotretinoin (IT-SLNs) and evaluate the ability of IT-SLNs to improve photostability, reduce skin permeation and irritating effects. IT-SLNs were prepared by the hot high pressure homogenization method. Size, zeta potential and morphological characteristics of the preparations were assessed by transmission electron microscopy (TEM) and thermotropic properties with differential scanning calorimetry (DSC). IT-SLNs had a small average diameter of 74.05 ± 8.91 nm and high encapsulation efficiency (EE) of 80.6 ± 1.2 %. The results showed that the entrapment of IT into SLNs reduced significantly its photodegradation. The in vitro permeation data showed that IT-SLNs can accumulate in the different layers of the skin and prevent systemic uptake of IT in mouse skin. IT-SLNs also significantly increased IT accumulation in the different layers of the stratum corneum of human skin. IT-SLN formulation was significantly less irritating compared to commercial IT-GEL, which shows its potential for improving skin tolerability and being a carrier for topical delivery of IT.


Author(s):  
Remya Pn ◽  
Damodharan N

Objective: The aim of the present investigation is to develop solid lipid nanoparticles (SLNs) of cilnidipine using hot homogenization followed by ultrasonication technique and to improve the dissolution characteristics of the drug.Methods: The cilnidipine-loaded SLNs were formulated using stearic acid (SA), glyceryl monostearate (GMS), and palmitic acid (PA) as lipid matrix and tween-20, tween-80, and tween-40 as an emulsifier by hot homogenization and ultrasonication method. The physicochemical characteristics of SLN were analyzed for Fourier transform infrared studies, entrapment efficiency (EE), zeta potential, in vitro drug release, particle size analysis, scanning electron microscopy, and stability.Results: The SLNs with PA showed a sustained release of drug 82%–88%, respectively, after 10 h. The SLNs of PA using tween-80 as emulsifier resulted with high EE% than SLNs of SA and GMS. The compatibility studies are done by Fourier transformed infrared for formulations which contain PA as lipid matrix and tween-80 as an emulsifier, and it showed no drug excipient incompatibility. The formulation containing PA and tween-80 shown particles of average size 152 nm having polydispersity index of. 217 with 68.7 % EE were produced. The zeta potential of the formulation was found to be – 27 mV and the order of percentage drug release was from PA>GMS>SA, and steric stabilizers retard the drug release more than ionic stabilizers.Conclusion: SLN formulations showed the best results in EE as well as in in vitro drug release and therefore confirmed that the novel drug delivery system provides an improved strategy for the treatment of hypertension.


Author(s):  
Vijaya R ◽  
Ram Kishan K R

Solid lipid nanoparticles (SLN) containing Disease Modifying Antirheumatic drugs (DMARDs) Methotrexate (MTX) and Doxycycline (DOX) was developed using a triglyceride (tristearin) and a polaxamer (pluronic F68). Hot homogenization of melted lipid and aqueous phase at temperature above the melting point of lipid had produced SLN dispersion. Optimization of process and formulation variables have yielded SLN having an entrapment efficiency of 65.07%±1.23% and 79.56%±0.92% for MTX and DOX respectively. Particle size and zeta potential measured using Malvern Zetasizer showed 157.2nm and -9.6mv respectively for the optimized SLN formulation. The compatibility between the drug and the formulation excipients was tested by Fourier Transform Infrared Spectroscopy (FTIR) and found to be compatible. Powder X-ray diffraction (PXRD) study revealed that the drugs and lipid were dispersed in crystalline state in SLN. The in vitro drug release studies performed in phosphate buffer of pH 7.4 using dialysis bag showed a sustained release of both the drugs (andgt;75%±1.4%) up to a period of two days. From the in vitro results, it can be concluded that SLN was found to be a suitable nano carrier for the incorporation of DMARDS: MTX and DOX without any significant interaction. The developed system produced sustained release of both the drugs (based on their concentration) for longer duration and thus suitable for the chronic inflammatory conditions of RA.


Author(s):  
Kishan V ◽  
Usha Kiranmai Gondrala ◽  
Narendar Dudhipala

Felodipine is an antihypertensive drug with poor oral bioavailability due to the first pass metabolism. For improving the oral bioavailability, felodipine loaded solid lipid nanoparticles (SLNs) were developed using trimyristin, tripalmitin and glyceryl monostearate. Poloxamer 188 was used as surfactant. Lipid excipient compatibilities were confirmed by differential scanning calorimetry. SLN dispersions were prepared by hot homogenization of molten lipids and aqueous phase followed by ultrasonication at a temperature, above the melting point. SLNs were characterized for particle size, zeta potential, drug content, entrapment efficiency and crystallinity of lipid and drug. In vitro release studies were performed in 0.1N HCl and phosphate buffer of pH 6.8 using dialysis method. Pharmacokinetics of felodipine-SLNs after oral admini-stration in male Wistar rats was studied. The bioavailability of felodipine was increased by 1.75 fold when compared to that of a felodipine suspension.  


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