Nanosystems L.l.c.

Elan Pharma International Limited

Sui-Ming Wong

Shuqian Xu

Stephen B Ruddy

Gary G Liversidge

Mary E Roberts

David A Engers

Eugene Rex Cooper

Alan R Pitt

Gregory L McIntire

Ian M Newington

Elaine M Liversidge

Jack M Shaw

Shugian Xu

The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increased rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1 (HIV-1) and type 2 (HIV-2) protease inhibitors are described.

Methods of treating mammals using nanocrystalline formulations of human immunodeficiency virus (HIV) protease inhibitors

The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increased rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1 (HIV-1) and type 2 (HV-2) protease inhibitors are described.

Methods of making nanocrystalline formulations of human immunodeficiency

The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increase rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1 (HIV-1) and type 2 (HIV-2) protease inhibitors are described.

Nanocrystalline formulations of human immunodeficiency virus (HIV)

There is disclosed a pharmaceutical composition which gels at physiological temperature. The composition is comprised of a block copolymer containing one or more polyoxyethylene blocks and one or more polyoxy (higher alkylene) blocks wherein at least some of the blocks are linked together by a linking group characterised in that the linking group is an oxymethylene group, and a therapeutic agent. The therapeutic agent is present as (i) nanoparticles of the therapeutic agent having the block copolymer adsorbed on the surface thereof, (ii) a suspension in a solution of the block copolymer, or (iii) as an aqueous solution in a solution of the block copolymer.

Pharmaceutical compositions containing polyalkylene block copolymers

The invention provides a novel compound having the structure ##STR1## wherein R is alkyl and R1, R2, R3 and R4 are each independently OCH3, H or I and n is 0 or 1 and m is 0 or 1. The compound is useful in a method of treating mammals either therapeutically or imaging mammals for diagnostic purposes. Useful therapeutic areas are in treating lymph nodes and tumors and diagnostic treatment is applicable to lymph nodes, tumors and in blood pool imaging. It is particularly advantageous to link an insoluble carrier molecule with a therapeutic or imaging agent to form the structure above. This makes the conjugate insoluble and thus amenable to forming nanoparticles.

Dual purposed diagnostic/therapeutic agent having a tri-iodinated

Dispersible particles consisting essentially of a crystalline drug substance having a surface modifier having the formula: ##STR1## wherein R is phenyl-(CH.sub.2).sub.10 CO or C.sub.12 H.sub.25 NHCO adsorbed on the surface thereof in an amount sufficient to maintain an effective average particle size of less than about 400 nm, methods for the preparation of such particles and dispersions containing the particles. Pharmaceutical compositions containing the particles exhibit unexpected bioavailability and are useful in methods of treating mammals.

Sugar base surfactant for nanocrystals

This invention provides a composition comprised of nanoparticles containing a therapeutic or diagnostic agent having a nonionic polymeric surfactant as a surface modifier adsorbed on the surface thereof, the surfactant being a block copolymer of ethylene oxide and butylene oxide and a method of making such nanoparticles. The compositions exhibit reduced macrophage uptake and improved toxicological profiles and facilitate particle size reduction such that milling time can be reduced and/or sterile filtration of the nanoparticles can be accomplished.

Butylene oxide-ethylene oxide block copolymer surfactants as stabilizer

This invention provides a composition comprised of nanoparticles containing a therapeutic or diagnostic agent having a block copolymer linked to at least one anionic group as a surface modifier adsorbed on the surface thereof and a method of making such nanoparticles. The compositions exhibit unexpectedly improved autoclave stability, reduced macrophage uptake, improved toxicological profiles and facilitate particle size reduction such that milling time can be reduced and/or sterile filtration of the nanoparticles can be accomplished.

Sulfated nonionic block copolymer surfactants as stabilizer coatings for

There is disclosed a composition containing nanoparticles having a surface modifier wherein the surface modifier is a block copolymer containing one or more polyoxyethylene blocks and one or more polyoxy(higher alkylene) blocks wherein at least some of the blocks are linked together by a linking group characterized in that the linking group is an oxymethylene group.

Growing community of inventors

Collegeville, PA, United States of America

Sui-Ming Wong