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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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Routes of Drug Administration: Parenteral01:25

Routes of Drug Administration: Parenteral

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The administration of drugs via parenteral routes allows for direct drug introduction into the systemic circulation, resulting in high bioavailability because the medication bypasses the harsh conditions of the gastrointestinal tract and hepatic metabolism.
The intravenous route (IV) of drug administration can be further categorized into two types. The bolus injection administers the entire dose rapidly, while an intravenous infusion slowly delivers smaller doses steadily.
The IV route is often...
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Drug Delivery: Miscellaneous Routes01:22

Drug Delivery: Miscellaneous Routes

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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.
Transdermal patches transport drugs...
329
Insulin Formulations: Types and Delivery01:27

Insulin Formulations: Types and Delivery

177
Insulin preparations are categorized by their duration of action into short-acting and long-acting types. Two strategies are used to modify insulin's absorption and pharmacokinetic profile: slowing the absorption post-subcutaneous injection, or altering human insulin's amino acid sequence or protein structure. These changes retain the insulin's ability to bind to the insulin receptor, but alter its behavior in solution or after injection.
Short-acting insulins are divided into...
177
Drug Delivery: Overview01:16

Drug Delivery: Overview

279
The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
279
Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics01:11

Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics

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All neuromuscular blocking agents are injected intravenously because they are poorly absorbed from the GI tract. Rapid onset is achieved with intravenous administration, although absorption is also adequate from an intramuscular injection. Since these agents are highly ionized, they do not readily penetrate cell membranes or cross the blood-brain barrier.
Instead, they are transported by the blood to different tissues. Muscles with a greater blood supply (arteries) and blood flow receive more...
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Injectable Supramolecular Polymer-Nanoparticle Hydrogels for Cell and Drug Delivery Applications
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Injectable dual thermoreversible hydrogel for sustained intramuscular drug delivery.

Fakhar Ud Din1, Jung Suk Kim2, Ho Cheol Lee2

  • 1College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea; Department of Pharmacy, Quaid-I-Azam University, Islamabad 45320, Pakistan.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|August 29, 2024
PubMed
Summary

A novel docetaxel-decorated solid lipid nanoparticle dual thermoreversible system (DCT-DRTS) offers improved intramuscular drug delivery. This system reduces burst release, provides sustained drug release, and enhances antitumor efficacy with better survival rates.

Keywords:
BioavailabilityBurst effectDocetaxelDual thermoreversible systemSolid lipid nanoparticlesSustained releaseTumor

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Area of Science:

  • Nanotechnology
  • Pharmaceutics
  • Oncology

Background:

  • Docetaxel is a potent chemotherapy agent with limitations in delivery and potential toxicity.
  • Solid lipid nanoparticles (SLNs) offer a promising platform for drug delivery, but require optimized formulations for specific administration routes.
  • Dual thermoreversible systems can enhance drug release profiles and improve therapeutic outcomes.

Purpose of the Study:

  • To develop and characterize a novel docetaxel-decorated solid lipid nanoparticle (DCT-SLN)-loaded dual thermoreversible system (DCT-DRTS) for intramuscular administration.
  • To evaluate the in vitro and in vivo performance of DCT-DRTS, focusing on reduced burst effect, sustained release, and improved antitumor efficacy.
  • To compare the efficacy of DCT-DRTS with conventional docetaxel formulations (hydrogel and suspension).

Main Methods:

  • Formulation of DCT-SLNs and their incorporation into a dual thermoreversible system with poloxamer.
  • Characterization of DCT-SLNs, including particle size (157 nm) and entrapment efficiency (93%).
  • In vitro drug release studies and in vivo antitumor efficacy evaluation in tumor cell xenograft models, including histopathological and immune-histochemical analyses.

Main Results:

  • DCT-SLNs exhibited a melting point around 32°C, facilitating gelation at physiological temperature within the dual thermoreversible system.
  • DCT-DRTS demonstrated sustained drug release and significantly reduced initial plasma concentration, overcoming the burst release effect observed with DCT-hydrogel.
  • Enhanced antitumor efficacy, improved survival rates, increased apoptosis, and reduced proliferation markers were observed in mice treated with DCT-DRTS.

Conclusions:

  • DCT-DRTS is a suitable formulation for intramuscular administration of docetaxel, offering sustained release and improved bioavailability.
  • The dual thermoreversible system effectively overcomes the burst release of docetaxel, leading to reduced toxicity.
  • DCT-DRTS shows significant potential for enhanced antitumor effects and improved patient outcomes in cancer therapy.