scholarly journals Intestinal Permeability of Artesunate-Loaded Solid Lipid Nanoparticles Using the Everted Gut Method

2018 ◽  
Vol 2018 ◽  
pp. 1-9 ◽  
Author(s):  
Wadzanayi L. Masiiwa ◽  
Louis L. Gadaga
Keyword(s):  
Drug Release ◽  
Intestinal Permeability ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Burst Release ◽  
Prolonged Release ◽  
Average Particle ◽  
Dissolution Profile ◽  
Dilution Technique ◽  
Solid Lipid

Background. Artesunate is one of the most potent, rapidly acting and therapeutically versatile antimalarial drugs. Its efficacy is hampered by poor aqueous solubility and stability resulting in low oral bioavailability. Recent efforts to nanoformulate artesunate have shown great potential of improving its dissolution profile and bioavailability. However, no study has yet been done to investigate the intestinal permeability of these nanoformulations, which is a critical determinant of systemic absorption. Objective of the Study. The main aim of the study was to determine the intestinal permeability of artesunate-loaded solid lipid nanoparticles (SLN). Method. The microemulsion dilution technique was used to fabricate artesunate-loaded solid lipid nanoparticles. In vitro drug release studies were performed at pH 1.2 and 6.8 using the dialysis membrane method. The everted gut sac method was used to assess the intestinal permeability of the prepared nanoparticles. Results. The average particle size was 1109 nm and the polydispersity index (PDI) was 0.082. The zeta potential was found to be −20.7 mV. The encapsulation efficiency of the solid lipid nanoparticles obtained was 51.7%. At both pH 1.2 and 6.8, pure artesunate was rapidly released within the first 30 mins while the SLN showed a biphasic release pattern with an initial burst release during the first hour followed by a prolonged release over time. The rate of drug release increased with increasing pH. The apparent permeability (Papp) of SLN was found to be greater (0.169 mg/cm2) as compared to that of pure artesunate (0.117 mg/cm2) at the end of the experiment. Conclusion. The results obtained in this study showed that the microemulsion dilution technique can be used to formulate artesunate solid lipid nanoparticles. The formulation exhibited a sustained drug release profile. The intestinal permeability of artesunate could be enhanced by the nanoformulation.

scholarly journals Fabrication, Characterization, and In Vivo Evaluation of Famotidine Loaded Solid Lipid Nanoparticles for Boosting Oral Bioavailability

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Muhammad Shafique ◽  
Mir Azam Khan ◽  
Waheed S. Khan ◽  
Maqsood-ur-Rehman ◽  
Waqar Ahmad ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Lipid Nanoparticles ◽  
Fickian Diffusion ◽  
Release Time ◽  
Pharmacokinetic Studies ◽  
Prolonged Release ◽  
Solid Lipid

Famotidine as H2 receptor has antagonistic effects on gastric secretion. Unfortunately, its hydrophobic nature contributes to its variable and poor oral bioavailability. In the current study efforts are being made to fabricate famotidine loaded solid lipid nanoparticles with narrow size distribution. Prepared nanoformulations were pharmaceutically evaluated to confirm the desired boosted oral bioavailability. Famotidine loaded nanoformulation (FFSe-4) showed particle size 111.9±1.3 nm, polydispersity index 0.464±0.03, zeta potential −33.46±2 mV, entrapment efficiency 84±2.7%, and drug loading capacity 2.709±0.13%. Drug-excipients compatibility was confirmed by Fourier transformed infrared spectroscopy. Scanning electron microscopy confirmed spherical shaped, nanosized particles. Differential scanning calorimetry and powder X-ray diffractometry confirmed the change in crystalline nature. Prepared nanoformulation was more stable at refrigerated temperature. In vitro study showed that drug release time is proportional to drug pay load and followed zero order kinetics. Release exponent (n>0.5) confirmed non-Fickian-diffusion mechanism for drug release. In vivo pharmacokinetic studies showed 2.06-fold increase in oral bioavailability of famotidine dispersed in solid lipid nanoparticles compared to commercial product. These results authenticate solid lipid nanoparticles as drug delivery system and propose prolonged release with improved oral bioavailability for famotidine.

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.

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.

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.

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

Vitamin A-loaded solid lipid nanoparticles for topical use: drug release properties

2000 ◽  
Vol 66 (2-3) ◽  
pp. 115-126 ◽  
Author(s):  
V. Jenning ◽  
M. Schäfer-Korting ◽  
S. Gohla
Keyword(s):  
Drug Release ◽  
Vitamin A ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Solid Lipid

Magnetic solid lipid nanoparticles co-loaded with albendazole as an anti-parasitic drug: Sonochemical preparation, characterization, and in vitro drug release

2018 ◽  
Vol 268 ◽  
pp. 11-18 ◽  
Author(s):  
Hassan Abidi ◽  
Mehrorang Ghaedi ◽  
Abdollah Rafiei ◽  
Ali Jelowdar ◽  
Anayatollah Salimi ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
In Vitro Drug Release ◽  
Solid Lipid ◽  
Magnetic Solid

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.

Development of Mupirocin- Tinidazole solid- Lipid Nanoparticles Loaded Topical gel for the Management of Bacterial Wound Infections

2021 ◽  
pp. 2785-2790
Author(s):  
Veintramuthusankar Veintramuthusankar ◽  
Pushparajudayakumar Pushparajudayakumar ◽  
Rajanduraibabyroselin Rajanduraibabyroselin
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Fickian Diffusion ◽  
Standard Drug ◽  
Topical Gel ◽  
Solid Lipid ◽  
Homogenization Technique ◽  
Significant Difference

Solid lipid nanoparticles (SLNs) are novel drug carrier system which consists of a solid matrix composed of a lipid being solid at both room and body temperatures with a mean Particle Size (PS) between 50 and 1000 nm Mupirocin -Tinidazole solid-lipid nanoparticles were prepared using hot homogenization technique using Glyceryl monosterate, Stearic acid, Tween 80 and Poloxamer 188 using hot homogenization technique. Size of the nanoparticles was in the range of 83 to 211 nm with the zeta potential values between -2.1 to -5.2. Atomic Force Microscopy (AFM) confirms the spherical shape of solid lipid nanoparticles. Entrapment efficiency was best in the F1 formulation. In vitro release of the pure drug was found to be 75% of mupirocin and 66.5% of tinidazole at the end of 1 hr. Drug release from SLNs dispersion followed Korsermeyrs peppas-model, indicating fickian diffusion drug release, while that from the gel followed non Fickian model drug release. Antibacterial activity of the SLNs was less but the SLNs based gel shows no significant difference in activity to that of standard drug gentamycin against aerobic bacteria. The SLNs dispersion exhibited physicochemical stability under refrigeration upto 45 days without significant difference in particle size. Best formulation was developed into a topical gel using sodium alginate and it was evaluated for pH, viscosity, spreadbility, extrudability, bloom strength, Minimum Inhibitory Concentration (MIC) and Methicillin resistant staphylococcus aureus (MRSA). Extrudability and spreadability parameters of the gel are similar to that of marketed Mupirocin 2% cream formulation

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