Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Ocular delivery of drugs

a technology for ocular delivery and drugs, applied in the field of new, can solve the problems of low ocular bioavailability of formulations, inconvenient ocular surface inflammation, and inability to optimally deliver restasis®, and achieve good stability, tolerability and bioavailability, and the effect of suitable ophthalmic compositions

Pending Publication Date: 2021-07-15
NANOMERICS
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The invention is about creating eye drop substances that are stable, tolerable, and can be easily absorbed by the eye. This is achieved by using special polymers that can assemble in water to form viscous or non-viscous substances with the added benefit of carrying drugs that can help treat eye conditions. These polymers are effective at carrying drugs without needing additional ingredients like lipids or emulsions. The size and concentration of the polymer molecules are important factors, with too small or too big polymers being less effective. A drug concentration below 2% also helps the polymer molecules absorb the drugs.

Problems solved by technology

In addition, inflammation of the ocular surface often occurs.
Due to the hydrophobicity and low aqueous solubility of CSA and TAC, they are generally formulated using oily vehicles which have been linked with bioavailability limitations, stability and ocular tolerance issues.
However, it is known that RESTASIS® is not optimal and the formulation suffers from low ocular bioavailability.
As a result, these compositions are prone to droplet coalescence which limit their shelf life.
In this respect, the release of CSA from the oily vehicles (castor oil emulsion or solution) was limited by the high partition coefficient of CSA in the oily phase.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Ocular delivery of drugs
  • Ocular delivery of drugs
  • Ocular delivery of drugs

Examples

Experimental program
Comparison scheme
Effect test

examples

[0085]Materials And Methods

[0086]Polymer

[0087]N-palmitoyl-N-monomethyl-N, Ndimethyl-N,N,N-trimethyl-6-O-glycolchitosan (GCPQ) was synthetized and characterized as previously described in I. F. Uchegbu, A. G. Schatzlein, X. Hou, Polymeric micellar clusters and their uses in formulating drugs, in, US20100159014 A1. The GCPQ used for the experiments had 20.51 Mol % of palmitoyl groups per monomer units, 11.93 Mol % of quaternary ammonium groups per monomer units, and a molecular weight of 9.13 KDa.

[0088]CsA Compositions

[0089]The composition containing CSA was prepared as follows. To a weighed sample of the polymer and weighed sample of the drug was added phosphate buffered saline (pH=7.4, 20 mL). The initial polymer, drug weight ratio was 7.5: 1 and the drug content was adjusted to give a concentration of 0.05%, 0.08% and 0.1% w / v. The liquid mixture was vortexed for two minutes to ensure complete mixing and subsequently subjected to high pressure homogenisation (Avestin Emulsiflex, GC...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
molecular weightaaaaaaaaaa
mean particle sizeaaaaaaaaaa
mean particle sizeaaaaaaaaaa
Login to View More

Abstract

The present invention relates to an aqueous composition comprising a macrolide immunosuppressant drug at a concentration of less than 2% w / v and an amphiphilic carbohydrate compound having a molecular weight in the range 1-50 kDa, for use in treatment of an eye disorder by topical application to the eye, wherein the amphiphilic carbohydrate compound is present at a concentration below 10% w / v of the composition. A preferred carbohydrate compound is quaternary ammonium palmitoyl glycol chitosan (GCPQ). Pharmaceutical compositions and methods of treatment are also provided. The treatment may be for instance dry eye syndromes (DES), vernal keratoconjunctivitis (VKC), eczema, atopic keratoconjunctivitis (AKC), Sjögren syndrome, post-operative refractive surgery, corneal transplant or contact lens intolerance.

Description

FIELD OF THE INVENTION[0001]The present invention relates to a new system for the ocular delivery of drugs.BACKGROUND TO THE INVENTION[0002]Topical ophthalmic formulations are generally used to treat diseases affecting the anterior portion of the eye including but not limited to glaucoma, iritis, conjunctivitis eye infection and dry-eye syndrome (DES). DES refers to a spectrum of ocular surface disorders having various aetiologies and is characterized by chronic eye dryness of the cornea and conjunctiva caused by the improper balance of tear production and drainage or an abnormality in the tear composition. In addition, inflammation of the ocular surface often occurs.[0003]A T-cell lymphocytes mediated inflammatory response has been recognized as a possible cause for DES. As a result, the use of Cyclosporine (CSA) and Tacrolimus (TAC) as topical immunosuppressants have emerged in recent years for the treatment of DES. Such treatments have been shown to decrease inflammatory response...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/00A61K38/13A61K9/08A61K47/36
CPCA61K9/0048A61K47/36A61K9/08A61K38/13A61P27/02A61P37/06A61P37/08
Inventor UCHEGBU, IJEOMASCHATZLEIN, ANDREASCAPRETTO, LORENZO
Owner NANOMERICS
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com