Nanostructured Lipid Carrier: A Potential System for Enhanced Oral Bioavailability of Felodipine

Candesartan Cilexetil (CC) is a prodrug widely used in the treatment of hypertension and heart failure, but it has some limitations, such as very poor aqueous solubility, high affinity to P-glycoprotein efflux mechanism, and hepatic first-pass metabolism. Therefore, it has very low oral bioavailability. In this study, glyceryl monostearate (GMS) and Capryol™ 90 were selected as solid and liquid lipids, respectively, to develop CC-NLC (nanostructured lipid carrier). CC was successfully encapsulated into NLP (CC-NLC) to enhance its oral bioavailability. CC-NLC was formulated using a hot homogenization-ultrasonication technique, and the physicochemical properties were characterized. The developed CC-NLC formulation was showed in nanometric size (121.6 ± 6.2 nm) with high encapsulation efficiency (96.23 ± 3.14%). Furthermore, it appeared almost spherical in morphology under a transmission electron microscope. The surgical experiment of the designed CC-NLC for absorption from the gastrointestinal tract revealed that CC-NLC absorption in the stomach was only 15.26% of that in the intestine. Otherwise, cellular uptake study exhibit that CC-NLCs should be internalized through the enterocytes after that transported through the systemic circulation. The pharmacokinetic results indicated that the oral bioavailability of CC was remarkably improved above 2-fold after encapsulation into nanostructured lipid carriers. These results ensured that nanostructured lipid carriers have a highly beneficial effect on improving the oral bioavailability of poorly water-soluble drugs, such as CC.

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Intra-articular delivery of a methotrexate loaded nanostructured lipid carrier based smart gel for effective treatment of rheumatic diseases

RSC Advances ◽

10.1039/c5ra22672d ◽

2016 ◽

Vol 6 (16) ◽

pp. 12913-12924 ◽

Cited By ~ 11

Author(s):

Chetan G. Shinde ◽

T. M. Pramod kumar ◽

M. P. Venkatesh ◽

K. S. Rajesh ◽

Atul Srivastava ◽

...

Keyword(s):

Effective Treatment ◽

Rheumatic Diseases ◽

Nanostructured Lipid Carrier ◽

Potential System

A nanostructured lipid carrier (NLC) based smart gel of methotrexate (MTX) was developed as a potential system for the treatment of rheumatic diseases (RD).

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Optimization of Nanostructured Lipid Carriers of Fenofibrate Using a Box-Behnken Design for Oral Bioavailability Enhancement

Current Drug Delivery ◽

10.2174/1567201818666210423110745 ◽

2021 ◽

Vol 18 ◽

Author(s):

Huijuan Wang ◽

Wei Hong ◽

Xiangyu Li ◽

Qian Jin ◽

Weifeng Yea ◽

...

Keyword(s):

Particle Size ◽

Oral Bioavailability ◽

Water Soluble ◽

In Vitro Dissolution ◽

Nanostructured Lipid Carrier ◽

Bioavailability Enhancement ◽

Box Behnken Design ◽

Predicted Values

Background: Fenofibrate (FNB) is a commonly used hypolipidemic agent. However, the oral bioavailability of FNB is limited by slow dissolution due to its low solubility. Thus, investigations on novel FNB formulations are necessary for their use. Objective: To enhance the oral bioavailability of FNB using optimized Nanostructured Lipid Carrier (NLC) formulations. Methods: Hot homogenization followed by ultrasonication was used to prepare FNB-NLCs. These formulations were optimized using a Box-Behnken design, where the amount of FNB (X1), a ratio of solid lipid/liquid lipid (X2), and the percentage of emulsifier (X3), were set as independent variables, while the particle size (Y1), and Entrapment Efficiency (EE%) (Y2), were used as dependent factors. An in vitro dissolution test was then performed using a paddle method, while an in vivo pharmacokinetic study of FNB-NLC formulation was performed in rats. Results: FNB-NLCs were successfully prepared and optimized using a Box-Behnken design. The particle size and EE% of the FNB-NLC had less than 5% difference from predicted values. The in vitro dissolution and oral bioavailability of the FNB-NLC were both higher than those of raw FNB. Results: FNB-NLCs were successfully prepared and optimized using a Box-Behnken design. The particle size and EE% of the FNB-NLC had less than 5% difference from predicted values. The in vitro dissolution and oral bioavailability of the FNB-NLC were both higher than those of raw FNB. Conclusion: A Box-Behnken design was successfully applied to optimize FNB-NLC formulation for the enhancement of the dissolution and bioavailability of FNB, a poorly water-soluble drug.

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Solidified nanostructured lipid carrier (S-NLC) for enhancing the oral bioavailability of ezetimibe

Journal of Drug Delivery Science and Technology ◽

10.1016/j.jddst.2019.101211 ◽

2019 ◽

Vol 53 ◽

pp. 101211 ◽

Cited By ~ 1

Author(s):

Ganesh Shevalkar ◽

Pradeep Vavia

Keyword(s):

Oral Bioavailability ◽

Nanostructured Lipid Carrier

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Enhanced Pharmacokinetic Activity of Zotepine via Nanostructured Lipid Carrier System in Wistar Rats for Oral Application

Pharmaceutical Nanotechnology ◽

10.2174/2211738508666200225113359 ◽

2020 ◽

Vol 8 (2) ◽

pp. 148-160 ◽

Cited By ~ 7

Author(s):

Cernam Tirumalesh ◽

Dinesh Suram ◽

Narendar Dudhipala ◽

Nagaraj Banala

Keyword(s):

Oral Bioavailability ◽

Oral Delivery ◽

Wistar Rats ◽

Water Solubility ◽

In Vitro Release ◽

Log P ◽

Nanostructured Lipid Carrier ◽

Vitro Release ◽

Sem Studies

Background: Zotepine (ZT) is a substituted dibenzothiepine tricyclic molecule and second generation antipsychotic drug. It is available as the parenteral and oral solid dosage form, but, orally administered ZT has a poor oral bioavailability (10%) that might be due to either poor water solubility, high lipophilicity (Log P 4) and also first-pass hepatic metabolism. Objective: The oral bioavailability of ZT was improved by loading into a nanostructured lipid carriers (NLCs) system. Methods: Hot homogenization with probe sonication method was used for the preparation of ZT-NLCs formulations and characterized for an optimal system based on physicochemical characteristics and in vitro release. Differential scanning calorimetry (DSC), X-ray diffraction (XRD) analysis, and scanning electron microscopy (SEM) studies were used to confirm the crystalline nature and shape of the optimized ZT-NLC formulation. The physical stability of the optimized ZT-NLC formulation was evaluated at the refrigerator and room temperature over two months. Furthermore, in vivo pharmacokinetic (PK) studies of optimized ZT-NLC and ZT coarse suspension (ZT-CS) as control formulation, were conducted in male Wistar rats. Results: The optimized formulation of ZT-NLC showed Z-avg, PDI, ZP of 145.8 ± 2.5 nm, 0.18 ± 0.05, -31.6 ± 1.8 mV, respectively. In vitro release studies indicated the sustained release of ZT. DSC and XRD studies revealed the conversion of ZT into an amorphous form. SEM studies showed the spherical shape of the ZT-NLC formulation. PK studies showed 1.8-folds improvement (p<0.05) in oral bioavailability when compared with ZTCS formulation. Conclusion: Overall, the results established that NLCs could be used as a new alternative delivery vehicle for the oral delivery of ZT.

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Rosuvastatin Loaded Nanostructured Lipid Carrier: For Enhancement of Oral Bioavailability

Indian Journal of Pharmaceutical Education and Research ◽

10.5530/ijper.50.4.13 ◽

2016 ◽

Vol 50 (4) ◽

pp. 605-611 ◽

Cited By ~ 4

Author(s):

Anand Panchakshari Gadad ◽

Swetha Gangadhar Tigadi ◽

Panchaxari Mallappa Dandagi ◽

Vinayak Shivamurthi Mastiholimath ◽

Uday Baburao Bolmal

Keyword(s):

Oral Bioavailability ◽

Nanostructured Lipid Carrier

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Enhancement of oral bioavailability of pentoxifylline by solid lipid nanoparticles

Journal of Liposome Research ◽

10.1080/08982100903161456 ◽

2009 ◽

Vol 00 (00) ◽

pp. 090820062440031-9 ◽

Cited By ~ 1

Author(s):

Jaleh Varshosaz ◽

Mohsen Minayian ◽

Elaheh Moazen

Keyword(s):

Solid Lipid Nanoparticles ◽

Oral Bioavailability ◽

Lipid Nanoparticles ◽

Solid Lipid

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Nanocochleates: innovative nanocarriers to enhance oral bioavailability of andrographolide

Planta Medica ◽

10.1055/s-0035-1565796 ◽

2015 ◽

Vol 81 (16) ◽

Author(s):

I Leto ◽

M Asprea ◽

MC Bergonzi ◽

A Karioti ◽

AR Bilia

Keyword(s):

Oral Bioavailability

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Photostability Study on Character and Antioxidant Activity of Tomato Extract (Solanum lycopersicum l.) in Nanostructured Lipid Carrier (NLC) and Conventional Creame

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v7i1.8919 ◽

2017 ◽

Vol 7 (1) ◽

Cited By ~ 1

Author(s):

Noorma Rosita ◽

Dewi Haryadi ◽

Tristiana Erawati ◽

Rossa Nanda ◽

Widji Soeratri

Keyword(s):

Antioxidant Activity ◽

Physical Stability ◽

Nanostructured Lipid Carrier ◽

Uvb Radiation ◽

K Value ◽

Antioxidant Power ◽

Solanum Lycopersicum L ◽

Tomato Extract ◽

Dpph Method ◽

High Shear Homogenization

The aim of this study was to investigate the ability of NLC in increasing photostability of tomato extract in term of antioxidant activity. Photostability testing on antioxidant activity of samples were conducted by accelerating method using UVB radiation 32.400 joule for 21 hours radiation. Antioxidant activity was measured by DPPH method. NLC was made by High Shear Homogenization (HPH) method at 24000 rpm for 4 cycles, while conventional creame was made by low speed at 400 rpm. The product were characterized include: pH, viscosity, and particle size. There were had difference characters and physical stability. NLC had smaller size, more homogenous and more stable than conventional creame. It was known that stability of antioxidant activity of tomato extract in NLC system higher than in conventional creame. That was showed with k value, as constanta of rate scavenging activity decreasing in antioxidant power between time (Sigma 2-tail less than 0.005) of NLC and conventional creame were: 2.03x10-2 %/hour ±0.08 (3.94) and 4.71x 10-2 %/ hour ±0.23 (4.88) respectively.

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