September 2016
Volume 57, Issue 12
Open Access
ARVO Annual Meeting Abstract  |   September 2016
Sustained Release Biodegradable Formulations for Intraocular Delivery: Extended Release of Hydrophilic APIs and Combination Products
Author Affiliations & Notes
  • Janet Tully
    Ophthalmology, Envisia Therapeutics, Moorisville, North Carolina, United States
  • Mari Yang
    Ophthalmology, Envisia Therapeutics, Moorisville, North Carolina, United States
  • Melissa Sandahl
    Ophthalmology, Envisia Therapeutics, Moorisville, North Carolina, United States
  • Stuart Williams
    Ophthalmology, Envisia Therapeutics, Moorisville, North Carolina, United States
  • Rhett Schiffman
    Ophthalmology, Envisia Therapeutics, Moorisville, North Carolina, United States
  • Footnotes
    Commercial Relationships   Janet Tully, Envisia Therapeutics (E); Mari Yang, Envisia Therapeutics (E); Melissa Sandahl, Envisia Therapeutics (E); Stuart Williams, Envisia Therapeutics (E); Rhett Schiffman, Envisia Therapeutics (E)
  • Footnotes
    Support  None
Investigative Ophthalmology & Visual Science September 2016, Vol.57, 4029. doi:
  • Views
  • Share
  • Tools
    • Alerts
      ×
      This feature is available to Subscribers Only
      Sign In or Create an Account ×
    • Get Citation

      Janet Tully, Mari Yang, Melissa Sandahl, Stuart Williams, Rhett Schiffman; Sustained Release Biodegradable Formulations for Intraocular Delivery: Extended Release of Hydrophilic APIs and Combination Products. Invest. Ophthalmol. Vis. Sci. 2016;57(12):4029.

      Download citation file:


      © ARVO (1962-2015); The Authors (2016-present)

      ×
  • Supplements
Abstract

Purpose : The ability to precisely manufacture poly(lactide-co-glycolide) (PLGA) and poly(lactide) (PLA) drug delivery systems for intraocular uses is limited by available technologies, specifically the ability to extend the release of hydrophilic, small-molecule APIs and API combinations within a single, fully biodegradable, implantable form factor. PRINT® ocular implants offer the ability to independently tune key product properties such as size, shape, needle fit, release rate, dose, API selection, biodegradation rate, as well as the ability to combine drugs. Herein we demonstrate the ability to control the extended release of hydrophilic APIs and API combinations within a single implant.

Methods : Specific size and shape biodegradable PLGA/PLA implants were fabricated with controlled loadings of a model hydrophilic API, timolol maleate, and with a combination of two APIs using proprietary PRINT technology. Implant size, shape and morphology were determined by Scanning Electron Microscopy (SEM). Drug loadings were measured by RP-HPLC. API release was characterized in vitro in 1X PBS, pH 7.4 with 0.1% Triton X-100 at 37C.

Results : Predefined size and shape biodegradable implants were fabricated using the PRINT technology with a high degree of mass uniformity and API content. In vitro release was controlled by tuning blends of polymers and excipients while retaining the shape, size and dose uniformity of the implant. Near zero-order release of fixed dose combinations of two APIs in a single implant was demonstrated over greater than 3 months in vitro. Multiple month sustained release was demonstrated with the model hydrophilic API, timolol maleate.

Conclusions : The PRINT technology uniquely allows for the fabrication of intraocular implants with uniform size, shape and dose. These formulations demonstrate the ability to control the rate of drug release of drug combinations in a single, fully biodegradable, implantable form factor. In addition, sustained release of hydrophilic APIs was demonstrated through the use of a model API, timolol maleate.

This is an abstract that was submitted for the 2016 ARVO Annual Meeting, held in Seattle, Wash., May 1-5, 2016.

 

Figure 1. A) Schemactic representation of combining two APIs with excipients to form specific size and shape implants (SEM micrograph). B) Near zero order release demonstrated from two model APIs in a single, fully biodegradable, implant. C) Sustained release of a hydrophilic small molecule, timolol maleate, for > 6 months.

Figure 1. A) Schemactic representation of combining two APIs with excipients to form specific size and shape implants (SEM micrograph). B) Near zero order release demonstrated from two model APIs in a single, fully biodegradable, implant. C) Sustained release of a hydrophilic small molecule, timolol maleate, for > 6 months.

×
×

This PDF is available to Subscribers Only

Sign in or purchase a subscription to access this content. ×

You must be signed into an individual account to use this feature.

×