Montelukast-loaded nanostructured lipid carriers: Part I Oral bioavailability improvement
Abstract
The purpose of the study was to formulate montelukast-loaded nanostructured lipid carrier (MNLC) to improve its systemic bioavailability, avoid hepatic metabolism and reduce hepatic cellular toxicity due to metabolites. MNLC was prepared using melt-emulsification-homogenization method. Preformulation study was carried out to evaluate drug-excipient compatibility. MNLCs were prepared using spatially different solid and liquid lipid triglycerides. CAE (DL-Pyrrolidonecarboxylic acid salt of L-cocyl arginine ethyl ester), a cationic, biodegradable, biocompatible surfactant was used to stabilize the system. MNLCs were characterized by FTIR, XRPD and DSC to evaluate physicochemical properties. MNLCs having a particle size of 181.4 ± 6.5 nm with encapsulation efficiency of 96.13 ± 0.98% were prepared. FTIR findings demonstrated no interaction between the drug and excipients of the formulation which could lead to asymmetric vibrations. DSC and XRPD study confirmed stable amorphous form of the montelukast in lipid matrix. In vitro release study revealed sustained release over a period of 24 h. In vivo single dose oral pharmacokinetic study demonstrated 143-fold improvement in bioavailability as compared to montelukast-aqueous solution. Thus, the result of this study implies that developed MNLC formulation be suitable to sustain the drug release with improvement in the bioavailability.
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Inhalable montelukast-loaded nanostructured lipid carriers improved systemic bioavailability (12-fold) and therapeutic outcomes compared to montelukast aqueous solutions.
“Inhalable montelukast-loaded nanostructured lipid carriers have been found to improve systemic bioavailability (12-fold) and eventual therapeutic outcomes compared to those of montelukast aqueous solutions.”
From Targeted therapy in chronic diseases using nanomaterial-based drug delivery vehicles (2019) · cites this paper as [174]
Inhalable drugs reduce dosing frequency, and bypassing first pass hepatic metabolism reduces hepatocellular toxicity.
“Inhalable drugs reduce dosing frequency, and bypassing the first pass hepatic metabolism reduces hepatocellular toxicity.173,174”
From Targeted therapy in chronic diseases using nanomaterial-based drug delivery vehicles (2019) · cites this paper as [174]
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- Authors
- Patil-Gadhe, A., & Pokharkar, V.
- Affiliations
- Bharati Vidyapeeth (Deemed to be University) (IN)
- Corresponding author
- Pokharkar, Varsha
- ORCID
- Pokharkar, Varsha
- Venue
- European Journal of Pharmaceutics and Biopharmaceutics
- Publisher
- Elsevier BV
- Published
- 2014-09
- Volume
- 88
- Issue
- 1
- Pages
- 160-168
- ISSN
- 0939-6411 (ISSN-L)
- OpenAlex
- W2050399519
- Cited by
- 107
- References
- 53
- Citations by year
- 2026: 1 · 2025: 5 · 2024: 7 · 2023: 12 · 2022: 6 · 2021: 17 · 2020: 10 · 2019: 15 · 2018: 9 · 2017: 9 · 2016: 9 · 2015: 6 · 2014: 1
- FWCI
- 4.72
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- European Journal of Pharmaceutics and Biopharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Keywords
- montelukast, nanostructured lipid carriers, oral bioavailability, amorphous drug delivery, cationic surfactants, drug-excipient compatibility, sustained drug release, pharmacokinetics, encapsulation efficiency
- MeSH terms
- Acetates, Animals, Asthma, Calorimetry, Differential Scanning, Chromatography, High Pressure Liquid, Cyclopropanes, Drug Carriers, Lipids, Male, Particle Size, Quinolines, Solubility, Sulfides, Surface-Active Agents, X-Ray Diffraction, Rats, Wistar, Spectroscopy, Fourier Transform Infrared, Area Under Curve, Microscopy, Electron, Transmission, Nanostructures, Rats, Nanoparticles
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