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Related Concept Videos

Drug Delivery: Parenteral Route01:29

Drug Delivery: Parenteral Route

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The parenteral route is a critical method of drug administration. It delivers compounds directly into the systemic circulation and bypasses the gastrointestinal tract. This approach is particularly advantageous for drugs that exhibit poor absorption or instability when administered orally.
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
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Drug Distribution: Tissue Binding01:21

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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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Drug Delivery: Miscellaneous Routes01:22

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Drug delivery methods like oral inhalation, nasal sprays, transdermal patches, eye drops, intravitreal injection,  and rectal administration provide localized effects with reduced toxicity.
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
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Local Anesthetics: Clinical Application as Spinal Anesthesia01:11

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Spinal anesthetics are given during lower abdomen and limb surgeries to block sensory and motor neurons. They are administered in the mid to low lumbar regions, primarily acting on the cauda equina's nerve roots. The blockade level depends on the local anesthetic (LA) concentration. Usually, low LA concentrations are sufficient to block sensory fibers, while only high LA concentrations block motor fibers. Other factors like injection volume and speed, the patient's posture, and the drug...
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Local Anesthetics: Clinical Application as Epidural Anesthesia01:29

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Epidural anesthetics are administered in the fat-filled epidural space, the outermost part of the spinal canal. This technique is commonly employed for pain management and anesthesia during lower abdomen and pelvis surgeries or labor and delivery.
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Choosing the appropriate route of drug administration is significantly influenced by two key factors: the therapeutic objectives and the inherent properties of the drug being used.
Administering drugs via inhalation allows for the direct delivery of gaseous, volatile substances or droplets to different parts of the respiratory tract. One of the advantages of the inhalation route is the rapid absorption of drugs into the circulatory system, which is possible because of the large surface area of...
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Drug retention after intradiscal administration.

Imke Rudnik-Jansen1,2,3, Jie Du1, Nina Karssemakers-Degen4

  • 1Department of Orthopedics, University Medical Center Utrecht, Utrecht, The Netherlands.

Drug Delivery
|October 20, 2024
PubMed
Summary

Drug retention in the intervertebral disc (IVD) is crucial for treating degeneration. Hydrophilic peptides cleared quickly, while hydrophobic drugs showed longer retention, especially with controlled-release microspheres in degenerative discs.

Keywords:
Drug retentionintervertebral disk degenerationpeptidepolyester amide microspheresmall molecule

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Area of Science:

  • Biomedical Engineering
  • Drug Delivery
  • Regenerative Medicine

Background:

  • Intervertebral disc degeneration (IVDD) treatment requires effective drug delivery.
  • Local IVD conditions and fluid exchange impact drug retention.
  • Optimizing therapeutics necessitates understanding drug clearance mechanisms.

Purpose of the Study:

  • To investigate the retention and release of hydrophilic peptides and hydrophobic small molecules within the intervertebral disc (IVD).
  • To compare drug retention in healthy versus degenerative IVDs.
  • To evaluate the efficacy of controlled-release microspheres for enhanced IVD drug delivery.

Main Methods:

  • Studied hydrophilic peptide (19F-P) release using 19F-NMR in a whole IVD culture model.
  • Visualized hydrophobic drug (IR-780) retention in rat IVDs using near-infrared imaging.
  • Assessed IR-780-loaded microsphere retention in IVDs, skin, and knee joints (OA model).

Main Results:

  • Most hydrophilic peptides cleared from the IVD within 7 days.
  • Hydrophobic drug retention in IVDs was longer than in skin or knee joints.
  • Degenerative IVDs showed higher drug retention with microsphere delivery compared to healthy IVDs.

Conclusions:

  • Clearance of peptides and hydrophobic molecules from the IVD is relatively rapid.
  • Controlled-release formulations are essential for sustained drug delivery to the IVD.
  • Anatomical location and local (patho)biology must guide therapeutic development for IVDD.