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Related Concept Videos

Site-Targeted Drug Delivery Systems: Polymeric Carriers01:24

Site-Targeted Drug Delivery Systems: Polymeric Carriers

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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...
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Transdermal Drug Delivery Systems01:18

Transdermal Drug Delivery Systems

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Transdermal drug delivery systems (TDDS) enable the controlled release of drugs across the skin into systemic circulation. They are particularly advantageous for drugs with short half-lives or narrow therapeutic indices, as they maintain consistent plasma concentrations and reduce the risk of subtherapeutic or toxic levels.TDDS are categorized into monolithic, reservoir, and mixed systems. Monolithic systems embed the drug in a polymer matrix, where diffusion governs release. Reservoir systems...
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Intrauterine Drug Delivery Systems01:21

Intrauterine Drug Delivery Systems

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Controlled-release systems for intravaginal and intrauterine drug delivery have been developed primarily for the administration of contraceptive steroid hormones. These delivery routes circumvent first-pass hepatic metabolism, thereby enhancing bioavailability and allowing for reduced systemic dosages compared to oral administration. Such approaches contribute to improved therapeutic efficacy and patient compliance, particularly in long-term contraceptive regimens.Intravaginal Drug Delivery...
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Modified-Release Drug Delivery Systems: Rate-Programmed II01:19

Modified-Release Drug Delivery Systems: Rate-Programmed II

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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...
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Ophthalmic Drug Delivery Systems01:23

Ophthalmic Drug Delivery Systems

97
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...
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Modified-Release Drug Delivery Systems: Site-Targeted01:24

Modified-Release Drug Delivery Systems: Site-Targeted

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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.
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Related Experiment Video

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Slow-release Drug Delivery through Elvax 40W to the Rat Retina: Implications for the Treatment of Chronic Conditions
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Polymer conjugated retinoids for controlled transdermal delivery.

Steven A Castleberry1, Mohiuddin A Quadir2, Malak Abu Sharkh3

  • 1Department of Chemical Engineering, Massachusetts Institute of Technology, Cambridge, MA 02139, United States; Koch Institute of Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, United States; Institute for Soldier Nanotechnologies, Massachusetts Institute of Technology, Cambridge, MA 02139, United States; Harvard-MIT Division of Health Sciences and Technology, Cambridge, MA 02139, United States.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|July 11, 2017
PubMed
Summary

This study introduces a novel pro-drug formulation for all-trans retinoic acid (ATRA) by bonding it to polyvinyl alcohol (PVA). This new topical delivery method reduces side effects and enhances ATRA accumulation in the skin for sustained release.

Keywords:
All-trans retinoic acidPoly (vinyl alcohol)Polymer conjugateTransdermal drug delivery

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Area of Science:

  • Dermatology
  • Materials Science
  • Drug Delivery

Background:

  • All-trans retinoic acid (ATRA) is used in cosmetics, acne treatments, and chemotherapy.
  • Current topical ATRA formulations (creams, emulsions) cause adverse effects due to rapid skin uptake.
  • Hydrophobic ATRA requires specific formulation strategies for effective topical delivery.

Purpose of the Study:

  • To develop a novel pro-drug formulation for sustained and controlled topical delivery of ATRA.
  • To mitigate the adverse side effects associated with conventional ATRA topical applications.
  • To enhance the accumulation and retention of ATRA within the skin layers.

Main Methods:

  • Covalently bonding ATRA to polyvinyl alcohol (PVA) via a hydrolytically degradable ester linkage.
  • Creating a water-soluble, amphiphilic nanomaterial for ATRA pro-drug formulation.
  • In vitro drug release studies and in vivo/ex vivo skin accumulation assessments.

Main Results:

  • The PVA-bound ATRA pro-drug demonstrated sustained release of active ATRA for up to 10 days in vitro.
  • Enhanced dermal accumulation of ATRA was observed in explant pig skin.
  • In vivo studies showed reduced application site inflammation compared to free ATRA.
  • The pro-drug formulation maintained measurable ATRA quantities at the application site for up to six days.

Conclusions:

  • The novel PVA-bound ATRA pro-drug offers a promising strategy for improved topical retinoid delivery.
  • This formulation effectively reduces skin irritation and enhances drug retention, leading to sustained therapeutic effects.
  • The developed nanomaterial facilitates controlled release and targeted accumulation of ATRA in the skin.