Dissolvable Ocular Insert Using Mucoadhesive Polymers for Prolonged Drug Residence
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Solution Overview
Problem
Current ocular drug delivery methods, such as eye drops, suffer from poor retention and short duration of action due to rapid drainage and binding to tear fluid proteins, leading to inefficient delivery of bioactive agents like olopatadine.
Innovation Solution
A dissolvable polymeric ocular insert comprising mucoadhesive polymers like hyaluronic acid and hydroxypropyl guar, along with olopatadine, is designed to release the drug and polymers slowly over an extended period, improving residence time and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If olopatadine is administered as eye drops, then the drug can be easily applied, but the drug is rapidly drained and has short residence time on the cornea
Solution Approach 1:
The ocular insert is placed in the inferior fornix before the drug needs to be released, allowing it to dissolve and release olopatadine over an extended period. This preliminary placement ensures the drug is delivered continuously rather than being rapidly drained like eye drops.
Solution Approach 2:
The biocompatible polymer matrix acts as an intermediary carrier that holds the olopatadine and releases it gradually. This polymer intermediary prevents the rapid drainage issue of eye drops while maintaining ease of application as a single insert unit.
2Duration of action of moving object
If LACRISERT® insert is used for extended drug delivery, then residence time is improved, but the insert remains in the eye for 15-20 hours causing blurred vision and discomfort
Solution Approach 1:
The insert is designed to dissolve completely within 4-8 hours by controlling the polymer composition and drug loading, rather than remaining for 15-20 hours. This parameter change in dissolution time eliminates blurred vision and discomfort while maintaining extended drug delivery.
Solution Approach 2:
The insert is placed locally in the inferior fornix rather than on the cornea, allowing drug delivery without interfering with vision. This local placement provides extended residence time without the harmful effects of corneal obstruction.
3Strength
If hydroxypropyl cellulose is used as polymer matrix, then the insert structure is maintained, but the slow dissolving properties lead to prolonged retention and side effects
Solution Approach 1:
The insert uses a composite polymer system combining hydroxypropyl cellulose with other biocompatible polymers in specific ratios. This composite formulation maintains structural integrity for proper placement while controlling dissolution to complete within 4-8 hours, avoiding prolonged retention side effects.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The ocular insert provides prolonged delivery of olopatadine and mucoadhesive polymers, enhancing symptom relief for both dry eye and ocular allergy, while minimizing side effects and improving patient compliance.
Implementation Method 1
The dissolvable ocular insert is a polymeric film... which comprises of at least two mucoadhesive polymers
Implementation Method 2
The dissolvable ocular insert... releases mucoadhesive polymers and olopatadine into the eye for an extended duration of time
Data Source
AI summary
An ocular insert, comprising: (a) at least one first mucoadhesive polymer selected from the group consisting of hyaluronic acid or sodium hyaluronate, polyvinylpyrrolidone, carboxyl methyl cellulose, and a combination thereof; (b) at least one second mucoadhesive polymer selected from the group consisting of hydroxyethyl guar, hydroxypropyl guar (HP-guar), hydroxypropyl methylcellulose (HPMC), and a combination thereof; (c) at least one plasticizer and (d) olopatadine in an amount from 2% to 20% by weight of the ocular insert, wherein the ocular insert has no visible recrystallization under examination with a polarized light microscope at approx. 100× magnification, wherein the ocular insert has a single-layer, homogeneous structure, wherein the at least one first mucoadhesive polymer and the at least one second mucoadhesive polymer are together present in the ocular insert in an amount of from about 75% to about 90% by weight of the ocular insert.