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.

FORMULATION AND EVALUATION OF SOLID LIPID NANOPARTICLES CONTAINING CAFFEINE TO TREAT CLINICAL MASTITIS

2020 ◽  
pp. 72-78
Author(s):  
AMRUTHA U ◽  
SUSHMITHA B ◽  
SHAIK RUBINA ◽  
PADMINI IRIVENTI
Keyword(s):  
Sustained Release ◽  
Solid Lipid Nanoparticles ◽  
Evaluation Studies ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Clinical Mastitis ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Solid Lipid

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.

scholarly journals Formulation and Evaluation of Solid Lipid Nanoparticles of Bifonazole

2020 ◽  
pp. 105-120
Author(s):  
Botre P.P ◽  
Maniyar M.G.
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Fungal Infections ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Gelling Agent ◽  
Rheological Parameters ◽  
Scanning Calorimetry ◽  
Solid Lipid

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.

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 Preparation, characterization and evaluation of moisturizing and UV protecting effects of topical solid lipid nanoparticles

2012 ◽  
Vol 48 (4) ◽  
pp. 683-690 ◽  
Author(s):  
Shiva Golmohammadzadeh ◽  
Mohsen Mokhtari ◽  
Mahmoud Reza Jaafari
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Morphological Characteristics ◽  
Lipid Nanoparticles ◽  
Uv Protection ◽  
Skin Hydration ◽  
Full Potential ◽  
Solid Lipid ◽  
Significant Difference

Solid lipid nanoparticles (SLN) were recently proposed as carriers for various pharmaceutical and cosmetic actives. These lipid nanoparticles can act as moisturizers and physical sunscreens on their own. Therefore, the full potential of these carriers has yet to be determined. The present study was aimed to determine and compare moisturizing and UV-protecting effects of different solid lipid nanoparticles (SLN) prepared by different solid lipids including Glyceryl monostearate (GMS), Precirol® (P) and cetyl palmitate (CP) as carrier systems of moisturizers and sunscreens. The influence of the size and matrix crystallinity of the solid lipids on the occlusive factor, skin hydration and UV-protection were evaluated by in vitro and in vivo methods. The SLN were prepared by high-shear homogenization and ultrasound methods. Size, zeta potential and morphological characteristics of the samples were assessed by transmission electron microscopy (TEM) and thermotropic properties with differential scanning calorimetry (DSC) technique. Results of the assessments showed that SLN-CP significantly increases skin hydration and UV-protection, compared to SLN-GMS and SLN-P. It was demonstrated that the size of SLN, crystallinity index of solid lipid in SLN and probably other mechanisms besides the occlusive factor can influence skin hydration and UV-protection indices. Furthermore, findings of the assessments demonstrated significant difference between in vitro and in vivo assessments regarding occlusive factor and moisturizing effects. Findings of the present study indicate that the SLN-CP could be a promising carrier for sunscreens and moisturizers.

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 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.

Licochalcone A-loaded solid lipid nanoparticles improve antischistosomal activity in vitro and in vivo

Nanomedicine ◽  
2021 ◽  
Author(s):  
Lívia Mara Silva ◽  
Danielle Gomes Marconato ◽  
Marcos Paulo Nascimento da Silva ◽  
Nádia Rezende Barbosa Raposo ◽  
Gabriela de Faria Silva Facchini ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Homogenization Method ◽  
Licochalcone A ◽  
Solid Lipid ◽  
Transmission Electron ◽  
High Shear Homogenization ◽  
Antischistosomal Activity

Aim: To isolate licochalcone A (LicoA) from licorice, prepare LicoA-loaded solid lipid nanoparticles (L-SLNs) and evaluate the L-SLNs in vitro and in vivo against Schistosoma mansoni. Materials & methods: LicoA was obtained by chromatographic fractionation and encapsulated in SLNs by a modified high shear homogenization method. Results: L-SLNs showed high encapsulation efficiency, with satisfactory particle size, polydispersity index and Zeta potential. Transmission electron microscopy revealed that L-SLNs were rounded and homogenously distributed. Toxicity studies revealed that SLNs decreased the hemolytic and cytotoxic properties of LicoA. Treatment with L-SLNs showed in vivo efficacy against S. mansoni. Conclusion: L-SLNs are efficient in reducing worm burden and SLNs may be a promising delivery system for LicoA to treat S. mansoni infections.

Formulation Development and Characterization of Solid Lipid Nanoparticles Containing Nimesulide

2009 ◽  
Vol 1 (1) ◽  
Author(s):  
Jain Pushpendra ◽  
Mishra Amit ◽  
Yadav K. ◽  
Patil K. ◽  
Baghel S.
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Average Diameter ◽  
Controlled Drug Release ◽  
Lipid Nanoparticles ◽  
Formulation Development ◽  
Solid Lipid

The aim of this study was to prepare nimesulide solid lipid nanoparticles (NIM-SLNs), to formulate the controlled drug release and to evaluate its physiochemical characteristics. NIM-SLNs were prepared by an emulsification and low-temperature solidification method. Additionally, attempts have been made to study the effect of individual process parameters (stirring speed and stirring time) and formulation parameters (Lecithin concentration, drug concentration and surfactant concentration) on entrapment efficiency. An approximately entrapment efficiency of (60%) and an average drug loading of (1.0 %) were achieved from optimized formulation of NIM-SLNs. The results show that the TMZ-SLNs had an average diameter of 187±1.23nm and in vitro drug release was conducted in phosphate-buffered saline (pH 7.4) at 37oC. The cumulative percentages drug release of nimesulide was found approximately 60% in 24 hours and release behavior was in accordance with Higuchi-equation. The results indicate that the SLNs is a promising controlled-release system. It may also allow a reduction in dosage and a decrease in systemic toxicity.

Preparation, Characterization and in vivo Evaluation of Felodipine Solid-Lipid Nanoparticles for Improved Oral Bioavailability

2015 ◽  
Vol 8 (4) ◽  
pp. 2995-3002
Author(s):  
Kishan V ◽  
Usha Kiranmai Gondrala ◽  
Narendar Dudhipala
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation ◽  
Solid Lipid

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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