scholarly journals Chinese White Wax Solid Lipid Nanoparticles as a Novel Nanocarrier of Curcumin for Inhibiting the Formation of Staphylococcus aureus Biofilms

Nanomaterials ◽  
2019 ◽  
Vol 9 (5) ◽  
pp. 763 ◽  
Author(s):  
Lin Luan ◽  
Zhe Chi ◽  
Chenguang Liu
Keyword(s):  
Staphylococcus Aureus ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Average Particle ◽  
Sustained Drug Release ◽  
Solid Lipid ◽  
Chinese White

Chinese white wax solid lipid nanoparticles (cwSLNs) were prepared by high shear homogenization and ultrasound methods. Using an optimized formula, spherical cwSLNs with an average particle size of 401.9 ± 21.3 nm were obtained. The cwSLNs showed high entrapment efficiency, approximately 84.6%, for loading curcumin. The curcumin loaded cwSLNs (Cur-cwSLNs) exhibited sustained drug release properties. Notably, Cur-cwSLNs had a higher drug release rate at pH 4.5 than at pH 7.4, which suggested their applicability in an acidic environment. Cur-cwSLNs were able to inhibit the growth of Staphylococcus aureus and were more effective at reducing the biofilms produced by this bacterium compared to free curcumin. This study confirmed that cwSLNs may be novel carriers for increasing the bioavailability of curcumin with the potential to inhibit the formation of S. aureus biofilms.

Preparation, Characterization and Optimization of Irbesartan Loaded Solid Lipid Nanoparticles for Oral Delivery

2021 ◽  
pp. 97-104
Author(s):  
Kumara Swamy S ◽  
Ramesh Alli
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Sustained Drug Release ◽  
Bioavailability Enhancement ◽  
Solid Lipid

The purpose of this study was to develop and evaluate irbesartan (IS) loaded solid lipid nanoparticles (SLNs; IS-SLNs) that might enhance the oral bioavailability of IS. IS, an angiotensin-receptor antagonist, used to treat hypertension. However, poor aqueous solubility and poor oral bioavailability has limited therapeutic applications of IS. Components of the SLNs include either of trimyristin/tripalmitin/tristearin/trilaurate/stearic acid/beeswax, and surfactants (Poloxamer 188 and soylecithin). The IS-SLNs were prepared by hot homogenization followed by ultrasonication method and evaluated for particle size, poly dispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), drug content and in vitro drug release. The physical stability of optimized formulation was studied at refrigerated and room temperature for two months. The optimized IS-SLN formulation (F4) had a mean diameter of about 217.6±3.62 nm, PDI of 0.163±0.032, ZP of -28.5±4.12, assay of 99.8±0.51 and EE of 93.68±2.47%. The formulation showed sustained drug release compared with control formulation over 24 h. Optimized formulation was found to be stable over two months. IS-SLN showed nearly spherical in shape using and converted to amorphous form by DSC. Thus, the results conclusively demonstrated SLNs could be considered as an alternative delivery system for the oral bioavailability enhancement of IS.

scholarly journals Statistical optimization of dithranol-loaded solid lipid nanoparticles using factorial design

2011 ◽  
Vol 47 (3) ◽  
pp. 503-511 ◽  
Author(s):  
Makarand Suresh Gambhire ◽  
Mangesh Ramesh Bhalekar ◽  
Vaishali Makarand Gambhire
Keyword(s):  
Particle Size ◽  
Factorial Design ◽  
Solid Lipid Nanoparticles ◽  
Ex Vivo ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Average Particle ◽  
Scanning Calorimetry ◽  
Solid Lipid

This study describes a 3² full factorial experimental design to optimize the formulation of dithranol (DTH) loaded solid lipid nanoparticles (SLN) by the pre-emulsion ultrasonication method. The variables drug: lipid ratio and sonication time were studied at three levels and arranged in a 3² factorial design to study the influence on the response variables particle size and % entrapment efficiency (%EE). From the statistical analysis of data polynomial equations were generated. The particle size and %EE for the 9 batches (R1 to R9) showed a wide variation of 219-348 nm and 51.33- 71.80 %, respectively. The physical characteristics of DTH-loaded SLN were evaluated using a particle size analyzer, differential scanning calorimetry and X-ray diffraction. The results of the optimized formulation showed an average particle size of 219 nm and entrapment efficiency of 69.88 %. Ex-vivo drug penetration using rat skin showed about a 2-fold increase in localization of DTH in skin as compared to the marketed preparation of DTH.

scholarly journals Surface Modification of Optimized Asenapine Maleate Loaded Solid Lipid Nanoparticles Using Box-Behnken Design

2021 ◽  
pp. 176-193
Author(s):  
A. Rekha Devi ◽  
M. Vidyavathi ◽  
S. P. Suryateja
Keyword(s):  
Surface Modification ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Brain Targeting ◽  
Average Particle ◽  
Box Behnken Design ◽  
Solid Lipid

Aim: The aim of the present study was to design and evaluate solid lipid nanoparticles of Asenapine maleate (<2% bioavailability) to enhance its oral bioavailability and surface modification for brain targeting. Methods: A modified solvent injection method was used to produce Asenapine maleate loaded solid lipid nanoparticles. A RSM 3-factor, 3-level Box-Behnken design was applied to study the effect of three independent variables, concentrations of lipid (A), drug (B) and surfactant (C) on three dependent variables, particles size (Y1), entrapment efficiency (Y2), and drug release (Y3). 3-D surface response plots were drawn and optimized formulation was selected based on desirability factor. Then it was coated with tween 80 for ease of permeability through blood brain barrier due to intact absorption of solid lipid nanoparticles. Results: The results of coated optimized formulation showed average particle size of 108.9 nm, entrapment efficiency of 78.62%, and in vitro drug release of 98.88±0.102% at 36 hr at pH 7.4. Morphologically, particles were almost spherical in shape with uniform size distribution. Targeting of coated optimized formulation to brain after oral administration was confirmed by fluorescence microscopy studies on male albino wistar strain rats. This research also envisaged that there is a >85% cell viability up to 125µg/ ml concentration of coated solid lipid nanoparticles by MTT assay. Conclusion: Thus, the current study successfully designed, developed an optimized SLN formulation of Asenapine maleate using a 3-factor, 3-level Box-Behnken design for brain targeting to treat Schizophrenia by bypassing the first pass metabolism with enhanced oral bioavailability.

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

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 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 TOPICAL SOLID LIPID NANOPARTICLES BASED GEL OF LAVENDER ESSENTIAL OIL FOR ANTI‑INFLAMMATORY ACTIVITY

2019 ◽  
pp. 175-182
Author(s):  
PALLAVI M CHAUDHARI ◽  
VAISHNAVI M BIND
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Essential Oil ◽  
Solid Lipid Nanoparticles ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Inflammatory Activity ◽  
Solid Lipid ◽  
Anti Inflammatory

Objective: The main objective of the study was to formulate and evaluate and perform an optimization study of lavender essential oil loaded solid lipid nanoparticles (SLNs) based gel. Materials and Methods: SLNs were prepared by the hot homogenization technique. A total of eight formulations were formulated as per 23 factorial design by design expert 11 software. The formulated SLNs were further evaluated for particle size, entrapment efficiency, drug release profile. After evaluation, the optimized batch was further used for formulating gel. The formulated gel was further subjected to ex vivo studies. Results: After the evaluation of all the parameters, batch 7 was found to be optimized. Batch 7 was found to have the lowest particle size of 30.91±0.30, higher entrapment efficiency of 89.99±0.87, and higher drug release of 90.41±0.55. It was further used for formulating gel which was found to be consistent, homogenous, smooth, and spreadable. The % inhibition of the formulated SLN based gel was found to be 28±0.1%. Conclusion: The SLNs were prepared and were formulated into the gel. The gel showed anti-inflammatory activity.

Development of Piroxicam loaded SLN-based Hydrogel for Transdermal Delivery

2014 ◽  
Vol 7 (1) ◽  
pp. 2238-2345
Author(s):  
Vinod Kumar Verma ◽  
Ram Alpana
Keyword(s):  
Drug Release ◽  
Transdermal Delivery ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Laser Scanning Microscopy ◽  
Diffusion Method ◽  
Solid Lipid

The aim of present study was to construct and investigate the efficacy of solid lipid nanoparticles (SLNs) based hydrogel for transdermal delivery of non-steroidal anti-inflammatory drug (NSAID) piroxicam. Solid lipid nanoparticles (SLNs) of piroxicam were produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs were composed of tripalmitin lipid, polyvinyl alcohol (PVA) as stabilizer, and solvent ethyl acetate. All the formulations were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were in nano-size range with maximum entrapment efficiency of 88.50±0.92. Further, Carbopol-934 was used as a gel matrix for preparation of hydrogel for improving the penetration rate across the skin and viscosity of piroxicam loaded SLNs for transdermal drug administration. The drug release behaviors from piroxicam loaded SLNs based hydrogel exhibited long duration and constant rate of drug release over 24 hr. Skin penetration of piroxicam loaded SLNs based hydrogel was assessed by confocal laser scanning microscopy (CLSM).

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.

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.

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