AI Article Synopsis

  • The pharmaceutical industry struggles with the low aqueous solubility of many drugs, making it challenging to deliver them effectively.
  • The study explored using water-miscible co-solvents, like PEG 400, alongside hydrogel-forming microneedles to enhance the transdermal delivery of poorly soluble drugs such as Nile red, olanzapine, and atorvastatin.
  • Results showed that co-solvents significantly improved the delivery rates, with over 83% of Nile red and about 50% of olanzapine and atorvastatin successfully permeating through neonatal porcine skin in 24 hours, indicating a promising method for better drug absorption.

Article Abstract

The poor aqueous solubility of existing and emerging drugs is a major issue faced by the pharmaceutical industry. Water-miscible organic solvents, termed co-solvents, can be used to enhance the solubility of poorly soluble substances. Typically, drugs with poor aqueous solubility and Log > 3 are not amenable to delivery across the skin. This study investigated the use of co-solvents as reservoirs to be used in combination with hydrogel-forming microneedles to enhance the transdermal delivery of hydrophobic compounds, namely Nile red, olanzapine and atorvastatin. A custom-made Franz cell apparatus was fabricated to test the suitability of a liquid drug reservoir in combination with polymeric microneedles. A co-solvency approach to reservoir formulation proved effective, with 83.30% ± 9.38% of Nile red dye, dissolved in 1 mL poly(ethylene glycol) (PEG 400), permeating neonatal porcine skin over 24 h. PEG 400 and propylene glycol were found to be suitable reservoir media for olanzapine and atorvastatin, with approximately 50% of each drug delivered after 24 h. This work provides crucial proof-of-concept evidence that the manipulation of microneedle reservoir properties is an effective method to facilitate microneedle-mediated delivery of hydrophobic compounds.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6920785PMC
http://dx.doi.org/10.3390/pharmaceutics11110605DOI Listing

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