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Topical compositions for the controlled delivery of proteins and peptides

A composition and protein technology, applied in the field of inhibiting, improving or treating human diseases, can solve the problems of unique biological properties, poor stability of developed molecules, etc.

Inactive Publication Date: 2011-04-27
KRINGLE PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although wound treatment products containing HGF have been investigated for nearly 20 years, the development of these products has been hampered by the molecule's poor stability and unique biological properties

Method used

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  • Topical compositions for the controlled delivery of proteins and peptides
  • Topical compositions for the controlled delivery of proteins and peptides
  • Topical compositions for the controlled delivery of proteins and peptides

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Some embodiments described herein include recombinant human hepatocyte growth factor (rhHGF) having the following sequence:

[0055] 1mwvtkllpal llqhvllhll llpiaipyae gqrkrrntih efkksakttl ikidpalkik

[0056] 61tkkvntadqc anrctrnkgl pftckafvfd karkqclwfp fnsmssgvkk efghefdlye

[0057] 121nkdyirncii gkgrsykgtv sitksgikcq pwssmipheh sflpssyrgk dlqenycrnp

[0058] 181rgeeggpwcf tsnpevryev cdipqcseve cmtcngesyr glmdhtesgk icqrwdhqtp

[0059] 241hrhkflpery pdkgfddnyc rnpdgqprpw cytldphtrw eycaiktcad ntmndtdvpl

[0060] 301etteciqgqg egyrgtvnti wngipcqrwd sqyphehdmt penfkckdlr enycrnpdgs

[0061] 361espwcfttdp nirvgycsqi pncdmshgqd cyrgngknym gnlsqtrsgl tcsmwdknme

[0062] 421dlhrhifwep dasklnenyc rnpdddahgp wcytgnplip wdycpisrce gdttptivnl

[0063] 481dhpviscakt kqlrvvngip trtnigwmvs lryrnkhicg gslikeswvl tarqcfpsrd

[0064] 541lkdyeawlgi hdvhgrgdek ckqvlnvsql vygpegsdlv lmklarpavl ddfvstidlp

[0065] 601nygctipekt scsvygwgyt glinydgllr vahlyimgne kcsqhhrgkv tlnese...

Embodiment 2

[0083] A dry powder containing dHGF with water absorbing capacity is produced. The manufactured composition contained approximately 2.5 μg dHGF, 37.8 g β-crystalline monoglyceride (1-glycerol monolaurate), 12.6 g β-crystalline monoglyceride (1-monomyristate) before drying. - glycerides), 48g hydroxyethyl cellulose (eg ), and the composition was brought up to 1200 mL of water.

[0084] A mixture of lipids in water was prepared in which monoglycerides, 1-glycerol monolaurate and 1-glycerol monomyristate were mixed with 200 g of water and heated to 70°C to 75°C. After mixing for 15 minutes at 70°C to 75°C, the lipid solution was slowly cooled to 20°C to 30°C to provide β-crystalline monoglycerides. Use the remainder of the water to dissolve the gel-forming compound, hydroxyethylcellulose (e.g. ), and dispersed dHGF. The three mixtures or solutions are mixed and spray dried to a final moisture content of less than 5% (eg frozen in a container with a bottom layer of liquid nit...

Embodiment 3

[0086] In other embodiments, a dry powder comprising only the gelling agent and monoglyceride is produced and reconstituted in a solution comprising dHGF (eg, a suitable buffer). The composition produced contained approximately 37.8 g 1-glyceryl monolaurate, 12.6 g 1-glycerol monomyristate, 48 g hydroxyethylcellulose (e.g. ), and the composition was brought up to 1200 mL of water.

[0087] A lipid mixture was prepared in which monoglycerides, 1-glycerol monolaurate and 1-glycerol monomyristate were mixed with 200 g of water and heated to 70°C to 75°C. After mixing for 15 minutes at 70°C to 75°C, the lipid solution was slowly cooled to 20°C to 30°C to provide β-crystalline monoglycerides. Use the rest of the water to dissolve hydroxyethyl cellulose (e.g. ). The two mixtures or solutions (ie the monoglyceride mixture and the hydroxyethylcellulose mixture) are then mixed and spray dried to a final moisture content of less than 5% (eg frozen in a container with a bottom layer...

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Abstract

Aspects of this invention relate to compositions and methods for the stabilization, storage, and delivery of biologically active agents, in particular peptides and nucleic acids. Particularly preferred embodiments include compositions that comprise a recombinant naturally occurring human hepatocyte growth factor (HGF), such as dHGF, a five amino acid truncated HGF variant, and at least one monoglyceride that remains in crystalline form at body temperature. Optionally, a gelling agent such as, hydroxyethylcellulose, and / or an antipathogenic compound (e.g., bupivacaine) can be included in the composition. Methods of use of these compositions to improve, ameliorate, or treat skin conditions are also embodiments.

Description

technical field [0001] Aspects of the invention relate to compositions and methods for stabilizing, storing and delivering proteins and peptides, particularly hepatocyte growth factor (HGF) and variants thereof, and using the stabilized compositions to inhibit, ameliorate or treat Methods of human diseases such as skin ulcers and skin cancer or precancerous conditions. Background technique [0002] Protein / peptide based drugs present unique problems of drug delivery. Proteins / peptides tend to denature in the gastrointestinal tract making oral administration unfavorable. Protein / peptide based drugs are therefore usually administered systemically in the form of sterile injectable solutions. Parenteral administration is also ineffective since proteins / peptides have a very short pharmacokinetic half-life in the bloodstream, are quickly metabolized and cleared. Therefore, many researchers have attempted to develop alternative methods to stabilize, store and deliver protein / pep...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00
CPCA61K38/00A61K9/1652A61K45/06A61K9/0014A61K9/1617A61K31/445C07K14/4753A61P17/00A61P17/02A61P35/00A61K2300/00
Inventor 阿克·林达尔
Owner KRINGLE PHARMA INC