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Advantages of liposome-based delivery system. Boost efficiency of ocular drug delivery Delivery of hydrophilic or lipophilic drugs Delivery of DNA/peptide/protein Liposome encapsulation may reduce ocular irritation. Criteria set forth by Lippomix. Within ocular pH range (6.8-7.6) Isotonic

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Advantages of liposome-based delivery system

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Advantages of liposome based delivery system l.jpg

Advantages of liposome-based delivery system

  • Boost efficiency of ocular drug delivery

  • Delivery of hydrophilic or lipophilic drugs

  • Delivery of DNA/peptide/protein

  • Liposome encapsulation may reduce ocular irritation


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Criteria set forth by Lippomix

  • Within ocular pH range (6.8-7.6)

  • Isotonic

  • Stable over the long term

    • Projection of Commercial Shelf Life

  • Pharmaceutically Elegant


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Formulation development

  • Formulation prototypes (44)

    -Buffered (24)

    -Unbuffered (20)

  • Formulations which meet criteria (11)

  • Short term stability data (1 month @ RT)

  • Summary

  • Conclusions


Formulation prototypes l.jpg

Unbuffered Formulations

0.9% NaCl

Phosphatidylcholine (PC)

Diclofenac

Benzalkonium or Benzethonium chloride

Buffered Formulations

Boric acid, pH 7.2

Phosphatidylcholine (PC)

Diclofenac

Benzalkonium or Benzethonium chloride

Formulation prototypes


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Liposomal formulation (placebo)

  • 0.1% (w/v) PC

  • 0.9% (w/v) NaCl


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Benzethonium chloride

FDA approved for ophthalmic use

Does not contain mercury

Maximum concentration of 0.01% (w/v)

Benzalkonium chloride

Commonly used, FDA approved preservative for multiple-use ophthalmic products

Does not contain mercury

Maximum concentration of 0.013% (w/v)

Anti-microbial agents


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Unbuffered Formulations: 0.9% NaCl (24)


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Recommended formulations: Unbuffered (6)


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pH Stability- Unbuffered formulations

  • No change in pH over a period of 30 days

  • pH of all six samples was between 6.5-7.0


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Particle size stability: Unbuffered formulations

  • No change in sample containing 0.3% PC and 0.1% diclofenac up to 20 days.

  • Five formulations increase in size after processing, but remain constant in size up to 20 days.


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Buffered Formulations: 0.3 M Boric acid, pH 7.2 (20)


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Recommended formulations:Buffered (5)


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pH Stability: Buffered Formulations

  • No change in pH over a 20 day period.

  • pH of all five formulations ranges from 7.2-7.3.


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Particle size stability: Buffered Formulations

  • During cooling of sample, all formulations shifted to a size ~3 m.

  • Microscopic estimates put the liposomes between 1-5 m.

  • The larger-sized particles appear to maintain their size over the short term.

  • Once a sample equilibrates, there is no change in particle size.


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Summary of findings

  • Formulations may be made buffered (boric acid) or unbuffered (NaCl).

  • PC concentrations within 0.05-0.3% (w/v) produce formulations with greatest clarity.

  • Diclofenac may be added at 0.02-0.1%.

  • Benzethonium chloride at 0.01% is the more suitable anti-microbial agent, with regard to formulation clarity.

  • pH of recommended formulations is constant over the short term (~30 days).

  • Most formulations shift to a larger particle size after processing, but remain stable once equilibrated.


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Formulation Criteria

  • Formulation clarity

  • Free of ethanol/organic solvents

  • Ability to include an anti-microbial agent

  • Within ocular pH range (6.8-7.6)

  • Isotonic

  • Stable over the long term (1 month to date)

    • Projection of Commercial Shelf Life

  • Pharmaceutically Elegant


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Conclusion

  • We can produce several liposome-based ophthalmic formulations of diclofenac.

  • All formulations are sterile, contain an anti-microbial agent, no organic solvents, and are within ocular pH and tonicity.

  • Furthermore, these formulations are stable with respect to clarity and pH .


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Future developments

Additional product opportunities:

  • Hydrophilic drugs

  • Lipophilic drugs

  • DNA/Proteins/Peptides

  • Other disease states (glaucoma, seasonal allergic or bacterial conjunctivitis, dry eye, etc…)


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pH Stability-Unbuffered Formulations


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pH Stability-Buffered Formulations


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