Cortisol palmitate liposomes: Enhanced anti-inflammatory effect in rats compared with free cortisol

Cleland, Leslie G.; Roberts, Barrie Vernon; Garrett, Robert A.; Allen, Theresa M.

doi:10.1007/bf01965402

Cited by 10 publications

(1 citation statement)

References 13 publications

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“…The degree and duration of antiarthritic activity of the liposomal drug was studied in arthritic rabbits [45]. The enhanced anti inflammatory effect of the liposomally entrapped cortisol palmitate over that of the free drug was also confirmed in the rat model [47]. The anti-inflammatory effect of the formula-tion was found to be much higher than that achieved by an equivalent dose of the microcrystalline drug.…”

Section: Cortisolmentioning

confidence: 99%

Use of Liposomal Drugs in the Treatment of Rheumatoid Arthritis

Chopra¹,

Gulati²,

Singh³

et al. 2008

CRR

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Rheumatoid arthritis is an autoimmune disease that results in joint deformity and disability. Conventional nonsteroidal anti-inflammatory drugs (NSAIDs), steroids and disease modifying antirheumatic drugs (DMARD's) are used for its treatment. Unconventional therapies, like enzyme oligodeoxy nucleotides, boron neutron capture therapy & radioisotopes are also being tried. The use of all these drugs is limited by a number of adverse effects. These side effects have been overcome to a large extent by the use of liposomes as delivery systems. This review presents rationale for the use of liposomes for the treatment of arthritis. Systemic as well as intra-articular delivery of liposome encapsulated anti-arthritic drugs is discussed. Success and limitations of this approach are also discussed by taking examples of different drug classes. PATHOPHYSIOLOGY OF RHEUMATOID ARTHRI-TISRheumatoid arthritis is initiated by an autoimmune response triggered by some unknown antigens. A self-reactive immune cell (a T or B cell programmed to attack a selfprotein) can be activated on infection with common bacteria or virus [3]. Several bacteria have been implicated in the initiation of rheumatoid arthritis including streptococcus, mycoplasma, borrelia and retrovirus.

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Section: Cortisolmentioning

confidence: 99%

Use of Liposomal Drugs in the Treatment of Rheumatoid Arthritis

Chopra¹,

Gulati²,

Singh³

et al. 2008

CRR

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Encapsulation of indomethacin in liposomes provides protection against both gastric and intestinal ulceration when orally administered to rats

Soehngen¹,

Godin-Ostro²,

Fielder³

et al. 1988

Arthritis & Rheumatism

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Encapsulation of indomethacin into egg phosphatidylcholine (EPC) monophasic vesicles (MPV) or into stable plurilamellar vesicles (SPLV) before oral administration to rats substantially reduced or eliminated the gastric and intestinal ulceration normally associated with ingestion of this drug. Ulcers were assessed by the 4-hour single-dose gastric ulceration model and the 4-or 14-day repeated-dose intestinal ulceration model, using microscopic/planimetric quantitation. Oral dosages of up to 10 mg/kg of indomethacin in polyethylene glycol400 resulted in substantial gastric ulceration, but not when given in methylcellulose suspension or as EPCMPV. Severe intestinal ulcers resulted following oral administration of indomethacin in either vehicle at daily 3-4-mg/kg doses, but did not result from EPCMPV formulations, whether dosed for 4 days or 14 days. Oral administration of pH-sensitive indomethacin liposomes constructed from cholesterol hemisuccinate resulted in loss of the protective action. Indomethacin-MPV showed both comparable bioactivity and comparable blood levels of the drug when contrasted with free drug in vehicles. Biodistribution studies demonstrated that when delivered from liposomes, drug and phospholipid are rapidly cleared through the stomach but then are differentially absorbed. Empty EPCMPV given by

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Drug Delivery Systems. 1. Site‐Specific Drug Delivery Using Liposomes as Carriers

Ranade

1989

The Journal of Clinical Pharma

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Drug delivery systems, offering controlled delivery of biologically active agents, are rapidly gaining importance in pharmaceutical research and development. To achieve controlled drug delivery, i.e., the administration of drugs so that optimal amount reaches the target site to cure or control the disease state, increasingly sophisticated systems containing different carriers have been developed. Macromolecules represent one of the carriers involved, and they have taken on a significantly prominent role in various modes of administration of therapeutic agents. Among macromolecules, for example, synthetic copolymers, polysaccharides, liposomes, polyanions and antibodies, as drug carriers, liposomes have proved most effective for diseases affecting the reticuloendothelial system and blood cells in particular. Liposomes, which are vesicles consisting of one or more concentrically ordered assemblies of phospholipids bilayers, range in size from a nanometer to several micrometers. Phospholipids such as egg phosphatidylcholine, phosphatidylserine, synthetic dipalmitoyl-DL-alpha-phosphatidylcholine or phosphatidylinositol, have been used in conjunction with cholesterol and positively or negatively charged amphiphiles such as stearylamine or phosphatidic acid. Alteration of surface charge has been shown to enhance drug incorporation and also influence drug release. Because of the multifold characteristics as drug carriers, liposomes have been investigated extensively as carriers of anticancer agents for the past several years. Liposomal entrapments include a variety of pharmacologically active compounds such as antimalarial, antiviral, anti-inflammatory and anti-fungal agents as well as antibiotics, prostaglandins, steroids and bronchodilators to name a few. The liposomal entrapment has been shown to have considerable effect on the pharmacokinetics and tissue distribution of administered drugs. Despite the potential value of liposomes as unique carriers, the major obstacles are the first order targeting of a systemically given liposomes, physical stability and manufacture of the liposomal products and these problems still remain to be overcome. Drug delivery systems evolving in the 1980s have become increasingly dependent on fundamental cell-biology and receptor-mediated endocytotic mechanisms. Drug delivery systems during the 1990s may take advantage of the specificity of receptor-mediated uptake mechanisms as well as polymer chemistry and cell-biology in order to introduce more precise and efficient target-specific delivery systems that are based especially on the liposome technology.

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Cortisol palmitate liposomes: Enhanced anti-inflammatory effect in rats compared with free cortisol

Cited by 10 publications

References 13 publications

Use of Liposomal Drugs in the Treatment of Rheumatoid Arthritis

Use of Liposomal Drugs in the Treatment of Rheumatoid Arthritis

Encapsulation of indomethacin in liposomes provides protection against both gastric and intestinal ulceration when orally administered to rats

Drug Delivery Systems. 1. Site‐Specific Drug Delivery Using Liposomes as Carriers

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