Liposomal-based formulation

Fielding, B. (1989). Drug delivery to the lungs and systemic circulation by inhalation of liposome based formulations, in Proc. 32nd Annual Meeting Western Pharmacology Society. Brecken-ridge, Colorado, January 1989. In Press. 

Barenholz Y, Amselem S. Quality control assays in the development and clinical use of liposome-based formulations. In Gregoriadis G, ed. Liposome Technology. Vol. 1. 2d ed. Boca Raton CRC Press, 1993 527-616. 

In Table 8.6 a summary is given of MAb and liposome-based formulations registered for cancer therapy. 

The mucoadhesion of the liposome-based formulations was examined both in vitro and in vivo. Using CLSM, the penetration of polymer-coated liposomes or polymer-liposome complexes into a layer of mucus in the rats after oral administration was confirmed. The pharmacological action of the model peptide drugs... 

Ugwu S et al (2005) Preparation, characterization, and stability of liposome-based formulations of mitoxantrone. Drug Dev Ind Pharm 31 223-229... 

Lei S et al (2004) Enhanced therapeutic efficacy of a novel liposome-based formulation of SN-38 against human tumor models in SCID mice. Anticancer Drugs 15 773-778... 

First liposome-based formulations Ambisome, Abelcet (1991)... 

Amphotericin B-induced ARF occurs in as many as 40% to 65% of patients treated with the conventional desoxycholate formulation.30 Nephrotoxicity is due to renal arterial vasoconstriction and distal renal tubule cell damage. Risk factors include high doses, treatment for at least 7 days, preexisting kidney dysfunction, and concomitant use of other nephrotoxic drugs.31 Three lipid-based formulations of amphotericin B have been developed in an attempt to decrease the incidence of ARF amphotericin B lipid complex, amphotericin colloidal dispersion, and liposomal amphotericin B. The range of... 

Wasserman V. Development, Characterization, Optimization, and Pharmacokinetic Evaluation of Liposome-Based Piperidine Nitroxide Formulation for Treatment of Pathological Conditions Tumor and Rheumatoid Arthritis. Ph.D. thesis, 2002. 

Table 1.1. Overview of some recently reported clinical studies on the application of liposome-based drug formulations.

Liposomal encapsulation or incorporation in a lipid complex can substantially affect a drug s functional properties relative to those of the unencapsulated or nonlipid-associated drug. Lipid-based formulations increase the circulation time and alter the biodistribution of associated amphotericin. Increasing drug levels at site of action and reducing levels in normal tissues offers 2 distinct clinical advantages An increased therapeutic index and altered toxicity profile relative to free drug. 

Additional naturally occurring lipids may be minor components of oral lipid-based formulations. Terpenes such as peppermint oil (>50% menthol) are fairly hydrophobic but can provide some solvent capacity. Steroids such as cholesterol, while important in topical and in parenteral liposomal products, are not important as oral pharmaceutical adjuvants. Phospholipids (e.g., egg or soybean phosphatidylcholine) an essential component of cell membranes, are considered polar lipids, and have surfactant properties. 

Liposome-Based Mucoadhesive Formulations for Oral Delivery of Macromolecules... 

A commercial product based on conventional liposomes has been introduced for the parenteral delivery of the anti-fungal drug, amphotericin B, which is poorly tolerated in conventional formulations. AmBisome, a liposomal formulation of amphotericin B, comprises SUV of diameter 50-100 ran. Two other lipid-based formulations of amphotericin B have also recently been commercially introduced ... 

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