In situ-Forming Pharmaceutical Organogels Based on the Self-Assembly of L-Alanine Derivatives

Couffin, Anne-Claude; Motulsky, Aude; Delmas, Pascal; Leroux, Jean‐Christophe

doi:10.1023/b:pham.0000019299.01265.05

Cited by 91 publications

(49 citation statements)

References 10 publications

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“…Over the past 6 years, we have been studying the ability of hydrophobized amino acids such as L-alanine [21] and L-tyrosine [22] to self-assemble in vegetable oils and form semi-solid/ solid systems at body temperature. In order to partially inhibit gelation at room temperature and allow the injection of the formulation, a small amount of N-methyl pyrrolidone (NMP), a biocompatible and water-soluble hydrophilic organic solvent [23], is added to the oil/ organogelators/drug mixture.…”

Section: Introductionmentioning

confidence: 99%

Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer’s disease

et al. 2010

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Organogels can be prepared by immobilizing an organic phase into a three-dimensional network coming from the self-assembly of a low molecular weight gelator molecule. In this work, an injectable subcutaneous organogel system based on safflower oil and a modified-tyrosine organogelator was evaluated in vivo for the delivery of rivastigmine, an acetylcholinesterase (AChE) inhibitor used in the treatment of Alzheimer's disease. Different implant formulations were injected and the plasmatic drug concentration was assayed for up to 35 days. In parallel, the inhibition of AChE in different brain sections and the biocompatibility of the implants were monitored. The pharmacokinetic profiles were found to be influenced by the gel composition, injected dose and volume of the implant. The sustained delivery of rivastigmine was accompanied by a significant prolonged inhibition of AChE in the hippocampus, a brain structure involved in memory. The implant induced only a minimal to mild chronic inflammation and fibrosis, which was comparable to poly(D,L-lactide-co-glycolide) in situ-forming implants. These findings suggest that tyrosine-based organogels could represent an alternative approach to current formulations for the sustained delivery of cholinesterase inhibitors.

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Section: Introductionmentioning

confidence: 99%

Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer’s disease

et al. 2010

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“…The main advantage of in situ forming gels is their injectability at room temperature. Once a drugcontaining gel is formed in situ, it could act as a sustained-release implant [47].…”

Section: Micromentioning

confidence: 99%

Organogels as a Potential Topical Drug Delivery System

Jha¹,

Maurya²

2018

Int J Drug Reg Affairs

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Semisolid preparations for external application to skin have gained much demand, since it is easily absorbed through the skin layers. Many novel topical dosage forms have been discovered, among which organogels appears to play an important role. Interest in organogels has increased in a wide variety of fields including chemistry, biotechnology and pharmaceutics. Organogels are thermodynamically stable, biocompatible, isotropic gel, which not only give localized effect, but also systemic effect through percutaneous absorption. Organogels are semi-solid systems, in which an organic liquid phase is immobilized by a three-dimensional network composed of self assembled, intertwined gelator fibers. The apolar phase gets immobilized within spaces of the three-dimensional networked structure formed due to the physical interactions amongst the self assembled structures of compounds regarded as gelators. Organogels have been explored as matrices for the delivery of bioactive agents. Compared to conventional topical dosage forms, these novel formulations are found to be more advantageous and efficient. In future, organogels can give way to many promising discoveries in the field of topical dosage forms. The current review aims at giving an idea about organogels, its applications and importance in topical delivery.

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“…Rheological studies [22]:-Rheological studies were performed with a thermostatically Fungilab Viscometer by using concentric cylinder spindle 61(L4) at 100 rpm and temperature 25o C. The results are given in table-1. Drug content: -The content of lornoxicam in the formulations was determined as per method described by Willimann and Luisi (1991) [23]. Accurately weighed gel (1g) was diluted with 100 ml of 0.1 N NaOH and analyzed spectrophotometrically at 376.5 nm for lornoxicam content and are shown in table-1.…”

Section: Characterization Of Organogelmentioning

confidence: 99%

Formulation and evaluation of lecithin organogel for treatment of arthritis

Jatav

Ramteke

2015

Int. J. Sci. World

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Background: Arthritis is a disease of the joint that involves inflammation of one or more joints. Topical administration of NSAIDs could deliver lornoxicam to the site of action in rheumatic diseases, which would reduce the gastrointestinal complications and side effects of the drug. Methods: In this method, the oily phase was prepared by dispersing the specific amount (ratio; 40:60) of purified lecithin at room temperature in isopropyl myristate as dispersing and emulsifying agent. The aqueous phase of polypropylene was prepared by dispersing a weighed amount of polypropylene and glycerol in water. It was stored at 2-4 oC overnight for the effective dissolution. The aqueous phase was slowly added in oily phase with stirring at 400 rpm using a mechanical stirrer. The prepared organogel of lornoxicam were evaluated for its appearance, organoleptic characteristic, viscosity, gelation temperature, drug content and in vitro release study. In vivo evaluation for analgesic activity of formulation was carried out in terms of skin irritation study, hot plate method; writhing test and edema paw induce method. Results: The drug content of organogel formulations was found in the range of 92.43±2.10-97.93±0.31% indicating uniform distribution of drug through the base and no interaction of drug with component of base. Posthoc Dunnet's ttest by employing statistical software, GraphPad InStat 3. It's shown differences between groups were considered significant at P < 0.05. Conclusion:The transdermal organogel formulation of lornoxicam could provide significant anti-inflammatory and antirheumatic activity when applied topically and was observed to be functional for topical delivery of lornoxicam.

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In situ-Forming Pharmaceutical Organogels Based on the Self-Assembly of L-Alanine Derivatives

Abstract: Low-molecular weight self-assembling organogelators may allow the preparation of novel in situ-forming hydrophobic implants.

Cited by 91 publications

References 10 publications

Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer’s disease

Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer’s disease

Organogels as a Potential Topical Drug Delivery System

Formulation and evaluation of lecithin organogel for treatment of arthritis

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