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Related Concept Videos

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

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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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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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Rate-programmed drug delivery systems (DDS) are designed to release drugs at specific, controlled rates to maintain consistent therapeutic levels. These systems are categorized based on their release mechanisms, including dissolution-controlled DDS, diffusion-controlled DDS, and combined dissolution-diffusion-controlled DDS.In dissolution-controlled DDS, the release rate depends on the slow dissolution of the drug itself or the surrounding matrix. Drugs with inherently slow dissolution rates,...
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Upon entering the systemic circulation, drugs can distribute into the interstitial and intracellular fluid of various tissue cells. This distribution is facilitated by the binding of drugs to different cellular components within tissues, which may lead to drug accumulation in specific areas. Drugs bound to tissue components serve as reservoirs that release free drugs back into the system, prolonging the drug's overall action. However, this accumulation can also result in local toxicity.
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Related Experiment Video

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Sodium Alendronate-Modified PLGA-mPEG Nanomicelles Loaded with Rifapentine for Targeted Delivery to Bone Tissue.

Weilin Wang1, Xin Cui1, Hengfa Wei1

  • 1State Key Laboratory of Pathogenesis, Prevention and Treatment of High Incidence Diseases in Central Asia, College of Pharmacy, Xinjiang Medical University, Urumqi 830054, China.

Pharmaceutics
|March 28, 2026
PubMed
Summary

A novel nanomicelle system functionalized with alendronate (ALN) enhances targeted delivery of rifapentine (RPT) to bone tissue. This bone-targeting drug delivery system shows improved efficacy and safety for treating bone tuberculosis.

Keywords:
bisphosphonatesbone targetingdrug delivery systempolymeric micellesrifapentine

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Area of Science:

  • Biomedical Engineering
  • Nanotechnology
  • Pharmacology

Background:

  • Conventional treatments for skeletal disorders like bone tuberculosis face challenges due to limited drug targeting and systemic toxicity.
  • Developing advanced drug delivery systems is crucial to improve therapeutic outcomes and reduce side effects.

Purpose of the Study:

  • To develop and evaluate an alendronate (ALN)-functionalized nanomicelle system for targeted delivery of rifapentine (RPT) to bone tissue.
  • To assess the bone-targeting efficiency, sustained-release properties, and safety profile of the novel nanomicelle formulation.

Main Methods:

  • Preparation and optimization of alendronate-poly(lactic-co-glycolic acid)-poly(ethylene glycol) (ALN-PLGA-mPEG) nanomicelles loaded with rifapentine (RPT).
  • Characterization of physicochemical properties, drug loading, encapsulation efficiency, and in vitro drug release.
  • Evaluation of in vivo bone-targeting efficacy using imaging, biodistribution studies, and histopathological examination.

Main Results:

  • Optimized ALN-PLGA-mPEG@RPT nanomicelles displayed a particle size of ~102 nm and a PDI of ~0.24.
  • The formulation achieved 16.74% drug loading and 50.27% encapsulation efficiency, with sustained RPT release over 12 hours.
  • In vivo studies demonstrated 1.93-fold higher drug accumulation in bone tissue compared to blood, with no observed organ toxicity.

Conclusions:

  • The ALN-PLGA-mPEG@RPT nanomicelle system effectively targets bone tissue and provides sustained drug release.
  • This nanomicelle formulation exhibits favorable biocompatibility, representing a promising strategy for treating bone tuberculosis and other skeletal diseases.