Novel Drug Delivery Systems

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Intro to Ophthalmic NDDS - Eye Spy New Ways

  • Ophthalmic NDDS: Advanced formulations/devices designed to optimize ocular drug delivery, overcoming limitations of traditional eye drops (e.g., rapid precorneal clearance).
  • Importance: Essential for effective management of anterior/posterior segment diseases, improving therapeutic outcomes.
  • Key Advantages:
    • ↑ Bioavailability, sustained drug levels.
    • ↓ Dosing frequency → ↑ patient adherence.
    • Targeted delivery, minimizing off-target effects.
    • Reduced systemic toxicity & local irritation.
  • Core Challenges:
    • Formidable ocular barriers (tear film, cornea, blood-ocular barriers).
    • Drug stability, sterility, biocompatibility.
    • Patient acceptance & cost-effectiveness.
  • Ocular drug delivery routes

⭐ Primary advantage: Enhanced bioavailability and reduced dosing frequency, leading to improved patient compliance and therapeutic efficacy.

Anterior Segment NDDS - Front Door Delivery

FeatureContact Lenses (CLs)Ocular Inserts (e.g., Ocusert)Punctal PlugsIn-situ Gels
FormDrug-eluting; soft/rigidSolid, polymeric; erodible/nonBiocompatible; occludes punctaLiquid → gel (pH, temp, ion trigger)
Mechanism↑ Contact time, sustained releaseCul-de-sac placement; prolonged useBlocks tear drainage; ↑ drug retention↑ Viscosity, ↑ precorneal residence time
Pros↑ Bioavailability, convenienceZero-order release, ↓ dosing freq.Minimally invasive, targetedEasy application, ↑ contact time
ConsLens issues, limited drug capacityForeign body sensation, expulsionExpulsion, irritationInitial blur, variable gelation
ExamplesGlaucoma, dry eye, antibiotic CLsPilocarpine (Ocusert), LacrisertDexamethasone insert, glaucoma plugsTimolol, Moxifloxacin gels

Posterior Segment NDDS - Backstage Pass Drugs

  • Key approaches to overcome barriers for drug delivery to retina/choroid.

Intravitreal drug delivery systems and release

SystemDelivery & DurationProsConsExamples
Intravitreal Inj.Direct bolus; Weeks-MonthsRapid onset, High local conc.Repeated, Endophthalmitis risk, IOP ↑Anti-VEGFs (Ranibizumab, Aflibercept)
Implants (Bio)Sustained release, degrades; MonthsNo removal needed, Predictable releaseInitial burst, InflammationOzurdex (Dexamethasone 0.7 mg)
Implants (Non-Bio)Sustained release, needs removal; Months-YearsLongest duration, Stable releaseSurgical removal, Fibrosis riskRetisert, Iluvien (Fluocinolone acetonide)
Particulate SystemsTargeted, sustained release; Variable (Days-Months)↑Bioavailability, ↓Toxicity, Cross barriersComplex manufacturing, Stability issuesLiposomes (Verteporfin), Nanoparticles

Emerging Ophthalmic NDDS - Eye‑Tech Horizons

  • Gene Therapy: Viral (AAV) & non-viral vectors for sustained intraocular drug production (e.g., anti-VEGF). Targets retinal dystrophies, AMD.
  • Cell-Based Delivery: Encapsulated Cell Technology (ECT) for continuous, long-term protein delivery.
  • Stimuli-Responsive Systems:
    • Smart Hydrogels: Drug release triggered by pH, temperature, light.
    • Nanocarriers: Nanoparticles, liposomes for targeted delivery, enhanced penetration.
  • Iontophoresis: Non-invasive transcorneal/transscleral drug delivery via electric current.
  • Microneedles: Minimally invasive arrays for precise suprachoroidal/intrascleral drug placement. Novel Ophthalmic Drug Delivery Systems

⭐ Microneedles enable minimally invasive suprachoroidal or intrascleral drug delivery, enhancing local efficacy and reducing systemic exposure.

High‑Yield Points - ⚡ Biggest Takeaways

  • Novel drug delivery systems (NDDS) enhance ocular bioavailability, prolong drug action, and improve patient compliance.
  • Examples: liposomes, nanoparticles, hydrogels, microneedles, and ocular inserts (e.g., Lacrisert).
  • Drug-eluting contact lenses provide continuous topical medication release.
  • Intravitreal implants (e.g., Retisert, Ozurdex) offer long-term therapy for posterior segment diseases.
  • Biodegradable polymers (e.g., PLGA) and non-biodegradable systems ensure sustained drug release.
  • Key challenges: overcoming ocular barriers (cornea, BRB) and rapid tear turnover.
  • Benefits include reduced dosing frequency and minimized systemic side effects.
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Practice Questions: Novel Drug Delivery Systems

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Ocular effects that include mydriasis are characteristic of which of the following drugs?

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Flashcards: Novel Drug Delivery Systems

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What drugs are used for the mainstay of treatment for uveitis?_____

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What drugs are used for the mainstay of treatment for uveitis?_____

Steroids and cycloplegics

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