scholarly journals Physicochemical characteristics and in vitro permeation of loratadine solid lipid nanoparticles for transdermal delivery

2020 ◽  
Vol 11 (11) ◽  
pp. 685-700
Author(s):  
Omar Sarheed ◽  
Douha Shouqair ◽  
KVRNS Ramesh ◽  
Muhammad Amin ◽  
Joshua Boateng ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Skin Permeation ◽  
Tween 80 ◽  
Physicochemical Characteristics ◽  
Lipid Nanoparticles ◽  
Water Addition ◽  
Oil Emulsion ◽  
Solid Lipid ◽  
Ultrasound Assisted

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.

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
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Tween 80 ◽  
Lipid Nanoparticles ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Release Agent ◽  
X Ray ◽  
Corneal Hydration ◽  
Solid Lipid

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.

scholarly journals Improved photostability, reduced skin permeation and irritation of isotretinoin by solid lipid nanoparticles / Povećana fotostabilnost, smanjena permeacija i iritacija izotretinoina iz kruto-tekućih nanočestica

2012 ◽  
Vol 62 (4) ◽  
pp. 547-562 ◽  
Author(s):  
Golmohammadzadeh Shiva ◽  
Mortezania Somaye ◽  
Jaafari Mahmoud Reza
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Skin Permeation ◽  
Mouse Skin ◽  
Morphological Characteristics ◽  
Average Diameter ◽  
Lipid Nanoparticles ◽  
Homogenization Method ◽  
Scanning Calorimetry ◽  
Solid Lipid

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.

scholarly journals FORMULATION, DEVELOPMENT, AND CHARACTERISATION OF CILNIDIPINE LOADED SOLID LIPID NANOPARTICLES

2018 ◽  
Vol 11 (9) ◽  
pp. 120
Author(s):  
Remya Pn ◽  
Damodharan N
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Tween 80 ◽  
Lipid Nanoparticles ◽  
Lipid Matrix ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Solid Lipid

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.

scholarly journals DEVELOPMENT AND EVALUATION OF CLOBETASOL–LOADED SOLID LIPID NANOPARTICLES FOR TOPICAL TREATMENT OF PSORIASIS

2019 ◽  
pp. 143-150 ◽  
Author(s):  
K. RAMESH REDDY ◽  
S. V. SATYANARAYANA ◽  
V. JAYASANKAR REDDY
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Drug Deposition ◽  
Solid Lipid ◽  
Prolonged Drug Release

Objective: The current research was structured to achieve a maximum topical delivery for the drug clobetasol-17-propionate (CP) and to predict the effects of various independent variables like lipid: drug ratio, surfactant, and homogenization time on particulate characters and performance solid lipid nanoparticles (SLNs). Methods: CP loaded SLNs were formulated by Emulsification–Homogenization method and optimized using 33 full factorial designs (Design-Expert software 11.0). Drug loaded SLNs were evaluated for various parameters like particle size, surface charge, polydispersity index, entrapment efficiency, surface morphology, thermal analysis, in vitro drug release through skin (Franz diffusion cell), drug deposition study and stability. Results: The optimized formulation (SLNs) attains a minimal Particle size of 133.3±3.66 nm, Poly dispersibility index of 0.179±0.081, % entrapment efficiency of 78.1±1.11 and Zeta potential of-36.2±0.11mV. Skin permeation study of CP loaded SLNs suspension showed prolonged drug release up to 24h. Maximum drug deposition was obtained after developing the drug into SLNs (48.22µg/ml) when compared to the pure drug (19.12µg/ml). Conclusion: SLNs were promising colloidal particulate carriers by which prolonged drug release and improved skin permeation was achieved for the drug Clobetasol 17- propionate.

scholarly journals In vivo Evaluation of Tazarotene Solid Lipid Nanoparticles Gel For Topical Delivery

2019 ◽  
Vol 11 (1) ◽  
Author(s):  
Rajkumar Aland ◽  
M. Ganesan ◽  
P. Rajeswara Rao
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Skin Permeation ◽  
Skin Irritation ◽  
Research Work ◽  
Topical Delivery ◽  
Lipid Nanoparticles ◽  
In Vitro Drug Release ◽  
Solid Lipid

The purpose of this research work was to develop and optimize the Solid Lipid Nanoparticles (SLNs) of Tazarotene for the effective topical delivery in the treatment of psoriasis. Tazarotene loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s design and based on the results further investigation was made 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, TEM, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. In vitro drug release of optimized SLN formulation (F1) was found to be 98.12 ± 1.52%, whereas pure drug release was 42.12 after 60 min. The optimized formulation was incorporated into the gel. The release rate (flux) of tazarotene across the membrane and excised skin differs significantly. The accumulative amount of Tazarotene in skin from SLN based gel formulation and marketed gel were 41.12 ± 0.12 mg and 30.02 ± 0.04 mg respectively. This result supported our hypothesis made in skin permeation studies on rat skin. From histopathological studies the microscopic observations indicate that the optimized SLN formulation, SLN based gel formulation and marketed gel has no significant effect on the microscopic structure of the skin. The skin-irritation studies indicated that SLN based gel containing Tazarotene did not show any sign of skin irritation as compared to moderate erythema shown by marketed gel formulation (Tazret® gel) after 72 h of application. Thus, SLN based gel formulation demonstrated advantage over marketed formulation in improving the skin tolerability of Tazarotene indicating their potential in improving patient acceptance and topical delivery of Tazarotene.

scholarly journals Effect of Lipids on Physicochemical Properties of Letrozole Loaded Solid Lipid Nanoparticles

2016 ◽  
Vol 8 (05) ◽  
Author(s):  
Archana Nerella ◽  
Basava Dontamsetti ◽  
Aruna Mantena
Keyword(s):  
Particle Size ◽  
Physicochemical Properties ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Physicochemical Characteristics ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Stabilizer Concentration ◽  
Vitro Release

The objective of the current investigation was to prepare solid lipid nanoparticles (SLNs) from different lipids and to study the effect of lipids on physicochemical characteristics of letrozole loaded SLN. In order to prepare small, stable, uniform and high Letrozole loaded SLNs, many factors such as lipid and stabilizer concentration and preparation parameters can be considered. Out of these, we have selected solid lipid as lipid matrix to investigate an effect on SLNs. SLNs were prepared using different lipids by modified hot sonication method. The effect of different lipids and stabilizers on physicochemical characteristics of Letrozole loaded SLNs were investigated. Letrozole loaded SLNs showed different physicochemical properties and release profiles according to used solid lipid. In case of particle size, SLN1 showed biggest particle size (532.5 ± 26.4nm) and highest encapsulation efficiency (81.37 ± 6.72%) and, SLN4 showed highest cumulative drug percentage (89.4 ± 1.8%, 24 h) release. These results suggest that lipids type affect physicochemical properties and release profile of SLN. The choice of lipid and stabilizer played important role on the physicochemical characteristics and in vitro release of Letrozole loaded SLNs.

Development of Solid Lipid Nanoparticles of Lamivudine for Brain Targeting

2009 ◽  
Vol 1 (1) ◽  
Author(s):  
Pravin Patil ◽  
Anil Sharma ◽  
Subhash Dadarwal ◽  
Vijay Sharma
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Rotation Speed ◽  
Lipid Nanoparticles ◽  
Brain Targeting ◽  
Brain Penetration ◽  
Solid Lipid ◽  
Diffusion Technique

The objective of present investigation was to enhance brain penetration of Lamivudine, one of the most widely used drugs for the treatment of AIDS. This was achieved through incorporating the drug into solid lipid nanoparticles (SLN) prepared by using emulsion solvent diffusion technique. The formulations were characterized for surface morphology, size and size distribution, percent drug entrapment and drug release. The optimum rotation speed, resulting into better drug entrapment and percent yield, was in the range of 1000-1250 r/min. In vitro cumulative % drug release from optimized SLN formulation was found 40-50 % in PBS (pH-7.4) and SGF (pH-1.2) respectively for 10 h. After 24 h more than 65 % of the drug was released from all formulations in both mediums meeting the requirement for drug delivery for prolong period of time.

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

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