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Site-Targeted Drug Delivery Systems: Polymeric Carriers01:24

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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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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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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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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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Related Experiment Video

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pH Modulation as a Key Strategy for Developing a Stable Lyotropic Liquid Crystal Formulation of Octreotide Acetate.

Yingshun Xin1, Shupei Yang1, Chan Li2

  • 1School of Pharmacy, Hebei Medical University, 361 East Zhongshan Road, Shijiazhuang 050017, China.

Pharmaceutics
|February 27, 2026
PubMed
Summary

Lyotropic liquid crystal (LLC) systems can deliver peptides effectively. Adjusting pH stabilizes octreotide acetate in LLC formulations, enabling sustained peptide delivery comparable to existing methods.

Keywords:
controlled releaselong-acting injectablelyotropic liquid crystaloctreotide acetatesubcutaneous injection

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Biotechnology

Background:

  • Lyotropic liquid crystal (LLC) systems offer sustained peptide delivery.
  • Octreotide acetate, a common salt form, poses stability challenges in LLC formulations.
  • Previous LLC formulations primarily used octreotide hydrochloride.

Purpose of the Study:

  • To investigate the formulation of octreotide acetate into stable LLC systems.
  • To determine the impact of pH adjustment on octreotide acetate stability in LLCs.
  • To evaluate the in vivo performance of the developed formulation.

Main Methods:

  • pH adjustment using 3M HCl-EtOH to approximately 5.7.
  • Stability assessment of octreotide acetate in LLCs at various temperatures and time points.
  • Structural analysis (mesophase identification) and in vivo pharmacokinetic studies in rats.

Main Results:

  • A stable LLC formulation of octreotide acetate was achieved via pH modulation.
  • High drug content (>90% at 40°C, >98% at 4°C) was maintained over extended periods.
  • In vivo studies confirmed sustained release and pharmacokinetic profiles comparable to octreotide hydrochloride LLCs.

Conclusions:

  • pH modulation is crucial for stabilizing octreotide acetate in LLC systems.
  • This strategy facilitates the use of clinically relevant peptide salt forms in LLC technology.
  • The findings support the broader application of LLCs for peptide therapeutics.