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Ophthalmic Drug Delivery Systems01:23

Ophthalmic Drug Delivery Systems

103
Ophthalmic drug delivery faces major limitations due to poor absorption across the corneal membrane. This process is primarily driven by diffusion and is influenced by two main factors: the physicochemical properties of the drug and tear drainage. Most ophthalmic drugs, such as pilocarpine, epinephrine, atropine, and local anesthetics, are weak bases. They are typically formulated at an acidic pH to enhance chemical stability. However, this leads to high ionization, reducing their ability to...
103
Site-Targeted Drug Delivery Systems: Polymeric Carriers01:24

Site-Targeted Drug Delivery Systems: Polymeric Carriers

63
Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
63
Modified-Release Drug Delivery Systems: Site-Targeted01:24

Modified-Release Drug Delivery Systems: Site-Targeted

51
Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
51
Modified-Release Drug Delivery Systems: Rate-Programmed II01:19

Modified-Release Drug Delivery Systems: Rate-Programmed II

54
Rate-programmed drug delivery systems release drugs in a controlled manner to maintain therapeutic levels. Three main designs include reservoir, matrix, and hybrid systems.Reservoir systems consist of a drug core enclosed within a membrane that controls drug release. In non-swelling reservoir systems, polymers like ethyl cellulose or polymethacrylates are used. These do not hydrate in aqueous media and control release through membrane thickness, porosity, or insolubility. This type includes...
54
Modified-Release Drug Delivery Systems: Stimuli-Activated01:30

Modified-Release Drug Delivery Systems: Stimuli-Activated

55
Stimuli-activated drug delivery systems are designed to release drugs in response to specific physical, chemical, or biological stimuli. These systems often utilize hydrogels—three-dimensional, hydrophilic polymer networks capable of swelling in aqueous environments and retaining significant fluid volumes. Upon exposure to particular stimuli, these hydrogels undergo structural transitions that allow the embedded drug to be released. Due to this adaptive behavior, such systems are also...
55
Modified-Release Drug Delivery Systems: Overview01:19

Modified-Release Drug Delivery Systems: Overview

69
Modified-release dosage forms are designed to address the limitations of drugs with short biological half-lives. These forms maintain stable therapeutic drug concentrations over extended periods, reducing the need for frequent dosing. A consistent drug level helps minimize peak-trough fluctuations, which can reduce adverse effects, lower the risk of drug resistance, and improve overall treatment effectiveness.One common type of modified-release form is the extended-release (ER) formulation. ER...
69

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Ocular Therapeutic Delivery and Advanced Tissue Retrieval in Adult Rats
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RES-loaded pegylated CS NPs: for efficient ocular delivery.

Saravanakumar Pandian1, Vinoth Jeevanesan1, Chandrasekar Ponnusamy1

  • 1Laboratory for Lipid Based Systems, Department of Pharmaceutical Technology, BIT Campus, Anna University, Tiruchirappalli 620 024, Tamil Nadu, India.

IET Nanobiotechnology
|May 7, 2017
PubMed
Summary

Researchers developed novel resveratrol-loaded, PEG-modified chitosan nanoparticles for glaucoma treatment. These nanoparticles demonstrated improved ocular delivery, reduced intra-ocular pressure, and good ocular tolerance in rabbit models.

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Area of Science:

  • Ophthalmology
  • Nanotechnology
  • Materials Science

Background:

  • Glaucoma is a leading cause of irreversible blindness worldwide, characterized by elevated intra-ocular pressure (IOP).
  • Effective drug delivery to ocular tissues remains a significant challenge due to biological barriers.
  • Resveratrol (RES), a natural polyphenol, possesses therapeutic potential for glaucoma, but its ocular delivery is limited.

Purpose of the Study:

  • To develop and characterize resveratrol (RES)-loaded polyethylene glycol (PEG)-modified chitosan (CS) nanoparticles (NPs) for glaucoma treatment.
  • To evaluate the ocular tolerance, permeation, and IOP-lowering efficacy of these novel NPs.

Main Methods:

  • Nanoparticles were formulated using the ionic gelation method with varying PEG concentrations.
  • Particle size, polydispersity index, entrapment efficiency, and drug loading were analyzed.
  • In vitro drug release, osmolality, ocular tolerance (hen's egg test), corneal permeation, and IOP reduction in rabbits were assessed.

Main Results:

  • Increasing PEG concentration increased particle size and PDI, while decreasing entrapment efficiency and RES loading.
  • Formulations exhibited controlled in vitro RES release and were iso-osmolar with tears.
  • PEG-modified CS NPs showed enhanced corneal permeation, reaching retinal tissues, unlike unmodified CS NPs.
  • RES-loaded PEG-modified CS NPs significantly reduced IOP by 4.3 ± 0.5 mmHg for up to 8 hours in normotensive rabbits.

Conclusions:

  • Developed RES-loaded PEG-modified CS NPs offer a promising approach for enhanced ocular drug delivery in glaucoma.
  • The nanoparticles demonstrated good ocular tolerance and effective IOP-lowering capabilities.
  • This novel nanocarrier system facilitates deeper ocular tissue penetration, suggesting potential for improved glaucoma management.