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

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.

scholarly journals DEVELOPMENT AND OPTIMIZATION OF TAZAROTENE LOADED SOLID LIPID NANOPARTICLES FOR TOPICAL DELIVERY

2019 ◽  
pp. 63-77
Author(s):  
RAJKUMAR ALAND ◽  
GANESAN M ◽  
RAJESWARA RAO P
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Lipid Nanoparticles ◽  
World Population ◽  
Transmission Electron Microscopy Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

Objective: Psoriasis is an unswervingly recurring, inflammatory, autoimmune disorder of the skin, disturbing about 2–5% of the world population. The main objective for this investigation is to develop and optimize the solid lipid nanoparticles (SLN) formulation of tazarotene for effective drug delivery. Methods: Tazarotene SLNs were fabricated by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency (EE). In view of the outcomes from the examinations of the responses acquired from Taguchi design, three diverse independent variables including sonication time (s), lipid to drug ratio (w/w), and surfactant concentration (%) were carefully chosen for further investigation utilizing central composite design. The lipid dynasan-116, surfactant poloxamer-188, and cosurfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, drug EE, zeta potential, in vitro drug release, and stability. Results: The prepared nanoformulations were evaluated for different parameters and 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, and the major mechanism of drug release follows zero-order kinetics release data for optimized formulation (F1) with non-Fickian (anomalous) with a strong correlation coefficient (R2=0.98598) of Korsmeyer-Peppas model. Transmission electron microscopy analysis has demonstrated the presence of individual nanoparticles in spherical shape, and the results were also compatible with particle size measurements. The drug content of tazarotene gel formulation was found to 98.96±0.021%, and the viscosity of gel formulation at 5 rpm was found to be 5.98×103±0.34×103 cp. The release rate (flux) of tazarotene across the membrane and expunged skin diverges pointedly, which specifies the barrier nature of skin. The flux value for SLN based gel formulation (193.454±4.324 μg/cm2/h) was found to be higher than that for marketed gel (116.345±2.238 μg/cm2/h). 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. Conclusion: From the obtained results, the topically oriented SLN-based gel formulation of tazarotene could be useful in providing effective and site-specific psoriasis treatment.

Effect of Acyclovir Solid Lipid Nanoparticles for the Treatment of Herpes Simplex Virus (HSV) Infection in an Animal Model of HSV-1 Infection

2019 ◽  
Vol 7 (5) ◽  
pp. 389-403 ◽  
Author(s):  
Ritika Kondel ◽  
Nusrat Shafiq ◽  
Indu P. Kaur ◽  
Mini P. Singh ◽  
Avaneesh K. Pandey ◽  
...  
Keyword(s):  
Particle Size ◽  
Single Dose ◽  
Drug Release ◽  
Mouse Model ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Proof Of Concept ◽  
In Vitro Drug Release ◽  
Solid Lipid

Background: Acyclovir use is limited by a high frequency of administration of five times a day and low bioavailability. This leads to poor patient compliance. Objectives: To overcome the problem of frequent dosing, we used nanotechnology platform to evaluate the proof of concept of substituting multiple daily doses of acyclovir with a single dose. Methods: Acyclovir was formulated as solid lipid nanoparticles (SLN). The nanoparticles were characterized for particle size, surface charge and morphology and in vitro drug release. The pharmacokinetic and pharmacodynamic of SLN acyclovir were compared with conventional acyclovir in a mouse model. Results: SLN showed drug loading of 90.22% with 67.44% encapsulation efficiency. Particle size was found to be of 131 ± 41.41 nm. In vitro drug release showed 100% release in SIF in 7 days. AUC0-∞ (119.43 ± 28.74 μg/ml h), AUMC0-∞ (14469 ± 4261.16 μg/ml h) and MRT (120.10 ± 9.21 h) were significantly higher for ACV SLN as compared to ACV AUC0-∞ (12.22 ± 2.47 μg/ml h), AUMC0-∞ (28.78 ± 30.16 μg/ml h) and MRT (2.07 ± 1.77 h), respectively (p<0.05). In mouse model, a single dose of ACV SLN was found to be equivalent to ACV administered as 400mg TID for 5 days in respect to lesion score and time of healing. Conclusion: The proof of concept of sustained-release acyclovir enabling administration as a single dose was thus demonstrated.

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

2020 ◽  
pp. 265-271
Author(s):  
REMYA P. N. ◽  
DAMODHARAN N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Stearic Acid ◽  
Palmitic Acid ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
In Vitro Drug Release

Objective: The aim of the present study is to develop solid lipid nanoparticles (SLNs) of Nimodipine using hot homogenization followed by ultrasonication technique and to improve the dissolution characteristics of the drug. Methods: The Nimodipine-loaded SLN was prepared using palmitic acid and stearic acid as a lipid matrix and Tween-80 as an emulsifier by a hot homogenization and ultra-sonication method. The physicochemical characteristics of SLN were investigated for entrapment efficiency, zeta potential, in vitro drug release, particle size analysis, Fourier transform infrared studies, scanning electron microscopy, and stability studies. Results: The mean particle size, PDI, Zeta potential and entrapment efficiency of optimized Nimodipine SLN formulation of stearic acid was found to be 119.54 nm, 0.165,-17.60mV, 85% and for palmitic acid was found to be 132.54 nm, 0.155,-17.0mV, 81% respectively. In vitro drug release studies indicated that after an initial burst release, SLN could provide prolonged release of Nimodipine. The selected SLNs have shown good stability for a period of 180 d. Conclusion: SLN formulations showed the best results in EE as well as in vitro drug release and therefore, these results indicate that SLN might be a promising delivery system to enhance the release of Nimodipine.

scholarly journals ZOLMITRIPTAN BRAIN TARGETING VIA INTRANASAL ROUTE USING SOLID LIPID NANOPARTICLES FOR MIGRAINE THERAPY: FORMULATION, CHARACTERIZATION, IN-VITRO AND IN-VIVO ASSESSMENT

2020 ◽  
pp. 86-93 ◽  
Author(s):  
DALIA A. ELATY MOSTAFA ◽  
MAHA K. A. KHALIFA ◽  
SAMEH. S. GAD
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Brain Targeting ◽  
Histopathological Study ◽  
Solid Lipid ◽  
The Brain

Objective: Zolmitriptan, a class of antidepressant drugs with poor bioavailability due to its first-pass metabolism. The aim of this study was to improve systemic bioavailability and explore the brain targeting impact of nasal Zolmitriptan (Zol) solid lipid nanoparticles (SLNs) gel for migraine treatment.  Methods: Stearic acid and cholesterol used as solid lipid and lecithin as a surfactant, emulsion solvent evaporation technique was used to produce Zolmitriptan SLNs. (Zol) SLNs were characterized for particle size, percent entrapment efficiency and in vitro drug release. Formula S6 showed greater percent entrapment efficiency (PEE), adequate particle size and sustained drug release behavior. Formula S6 was integrated into HPMC gel (3%) to prepare nasal gel. Zol SLN nasal gel was subjected to histopathological study to ensure brain targeting.  Results: It was observed that all prepared Zol SLNs were in the nano-sized range with a polydispersity index of<0.5. In the cholesterol/lecithin combination, higher PEE%, better stability, and less agglomeration inclination were discovered. Results of the release profiles showed that developed Zol-SLNs were able to release Zolmitriptan in a sustained manner. Histopathological study of the brain tissues showed that Zolmitriptan SLN nasal gel can reach brain cells and localized for 24 h although the hydrophobicity of the target drug. Conclusion: Intranasal administration of Solid lipid nanostructure of Zolmitriptan through the olfactory pathway in which it travels from the nasal cavity to brain tissue achieved drug targeting potential of about 90% compared with conventional Zolmitriptan tablets. The small particle size helped them to squeeze themselves through the small opening in the olfactory neurons to the brain via different endo-cystic pathways of neuronal cells in nasal tissue membranes.

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 Transdermal delivery of solid lipid nanoparticles of ketoprofen for treatment of arthritis

2019 ◽  
Vol 8 (3) ◽  
pp. 627-636
Keyword(s):  
Drug Release ◽  
Transdermal Delivery ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Controlled Drug Release ◽  
Lipid Nanoparticles ◽  
In Vitro Drug Release ◽  
Solid Lipid ◽  
Anti Inflammatory

Ketoprofen (KP) is a 2-(3-benzolphenyl) propionic acid with anti-inflammatory, analgesic and antipyretic properties. It belongs to BCS Class II drug. It also has a short half-life of 120 minutes. Drugs acidic nature causes gastric irritation which is a major limitation. The present work aims to develop and evaluate solid lipid nanoparticles (SLN) to provide transdermal drug delivery. SLN loaded gel will enhance the solubility of Ketoprofen thereby increasing bioavailability giving controlled drug release. Solid lipid nanoparticles were prepared by solvent injection followed by probe sonication method. Cetyl palmitate was used as lipid and Tween80 as a surfactant. Batches were prepared by varying the concentration of the lipid phase and the surfactant phase. The solid lipid nanoparticles were evaluated for particle size analysis, drug entrapment efficiency, zeta potential and in vitro drug release study. Differential scanning calorimetry (DSC) and Powder X-ray diffraction (PXRD) study were done to study crystallinity behavior.SLN was studied for its anti-inflammatory activity. F4 batch of SLN was incorporated into gel and evaluated for drug content, pH, viscosity, in-vitro diffusion and ex-vivo diffusion study. SLN were successfully prepared. Among the batches F1-F9, F4 batch was selected based upon the size, entrapment efficiency, stability and drug release. The resultant solid lipid nanoparticles showed entrapment efficiency of 78.24%. The solubility was improved by 50 fold. The particle size was 250 nm, PDI was 0.398 and zeta potential -21.98mV. In-vitro drug release of gel from F4 SLN batch showed controlled drug release in 8 hours. Transdermal delivery of SLN retaining its anti-inflammatory activity was successfully developed.

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-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. 

scholarly journals FORMULATION AND CHARACTERIZATION OF PAPAIN LOADED SOLID LIPID NANOPARTICLES AGAINST HUMAN COLORECTAL ADENOCARCINOMA CELL LINE

2018 ◽  
Vol 11 (10) ◽  
pp. 393
Author(s):  
Suriyakala Perumal Chandran ◽  
Kannikaparameswari Nachimuthu
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Cell Viability ◽  
Cell Line ◽  
Solid Lipid Nanoparticles ◽  
Colorectal Adenocarcinoma ◽  
Lipid Nanoparticles ◽  
In Vitro Drug Release

Objective: Colorectal cancer is one of the most commonly diagnosed cancer and also most common gastrointestinal malignancy with high prevalence rate in the younger population. Usually, cancer cells are surrounded by a fibrin coat which is resistant to fibrinolytic degradation. This fibrin coat is act as self-protective against natural killing mechanism. The main objective was to prepare papain-loaded solid lipid nanoparticles (P-SLN) by melt dispersion-ultrasonication method and investigated the cytotoxic efficacy against colorectal adenocarcinoma (human colorectal adenocarcinoma [HCT 15]) cells.Methods: Optimized polymer ratio was characterized by differential scanning calorimetry, Fourier-transform infrared, X-ray diffraction, scanning electron microscopy, entrapment efficiency, particle size and zeta potential analysis, in vitro drug release, and in vitro cytotoxicity studies on HCT-15 colorectal adenocarcinoma cells.Results: The results showed that the particle size, morphological character and zeta potential value of optimized batch P-SLN were 265 nm, spherical and −26.5 Mv, respectively. The in vitro drug profile of P-SLN exhibited that it produced sustain drug release, and the cell viability of HCT-15 against P-SLN shown better efficacy than pure papain enzyme.Conclusion: P-SLNs were successfully prepared and investigated the in vitro drug release and in vitro cell viability against HCT-15 cell line.

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