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Transdermal Drug Delivery Systems

Transdermal Drug Delivery Systems

Transdermal drug delivery systems (TDDS) enable the controlled release of drugs across the skin into systemic circulation. They are particularly advantageous for drugs with short half-lives or narrow therapeutic indices, as they maintain consistent plasma concentrations and reduce the risk of subtherapeutic or toxic levels.TDDS are categorized into monolithic, reservoir, and mixed systems. Monolithic systems embed the drug in a polymer matrix, where diffusion governs release. Reservoir systems...

Drug Delivery: Overview

Drug Delivery: Overview

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 gastrointestinal...

Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence

Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence

Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...

Formulation and Manufacturing Process: Physical Attributes of Generic Tablets and Capsules

Formulation and Manufacturing Process: Physical Attributes of Generic Tablets and Capsules

Bioequivalence in generic drugs, such as tablets and capsules, refers to their pharmaceutical equivalence to the brand-name counterparts. However, for therapeutic equivalence, manufacturers must also consider physical attributes like size, shape, and weight (FDA Guidance for Industry, December 2003). Discrepancies in these aspects could impact patient compliance and cause medication errors. For instance, swallowing difficulties, often experienced with larger tablets or capsules, can lead to...

Modified-Release Drug Delivery Systems: Influencing Factors

Modified-Release Drug Delivery Systems: Influencing Factors

Modified-release drug delivery systems are designed to optimize the therapeutic effect of drugs by minimizing side effects, reducing the dosage required, and controlling drug release to align with pharmacokinetic and pharmacodynamic needs. The system depends on two key factors: the drug's release from the formulation and its movement through the body to the target site. Unlike conventional dosage forms, where absorption is the limiting step, the rate of drug release is the key determinant in...

Modified-Release Drug Delivery Systems: Overview

Modified-Release Drug Delivery Systems: Overview

Modified-release dosage forms are designed to address the limitations of drugs with short biological half-lives. These forms maintain stable therapeutic drug concentrations over extended periods, reducing the need for frequent dosing. A consistent drug level helps minimize peak-trough fluctuations, which can reduce adverse effects, lower the risk of drug resistance, and improve overall treatment effectiveness.One common type of modified-release form is the extended-release (ER) formulation. ER...

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Updated: May 31, 2026

Fentanyl Analog Screening using LC-TIMS-TOF MS/MS

Fentanyl Analog Screening using LC-TIMS-TOF MS/MS

Published on: November 8, 2024

Formulation issues associated with transdermal fentanyl delivery.

P Santos¹, A C Watkinson, J Hadgraft

¹Department of Pharmaceutics, University of London, London, UK.

International Journal of Pharmaceutics

|July 5, 2011

Summary

This summary is machine-generated.

Supersaturated fentanyl formulations enhance transdermal drug delivery across human skin. Stabilizing these formulations is key, as drug crystallization impacts finite dose delivery effectiveness.

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Fentanyl Analog Screening using LC-TIMS-TOF MS/MS

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Published on: November 8, 2024

Visualizing and Quantifying Pharmaceutical Compounds within Skin using Coherent Raman Scattering Imaging

Visualizing and Quantifying Pharmaceutical Compounds within Skin using Coherent Raman Scattering Imaging

Published on: November 24, 2021

Area of Science:

Pharmaceutical Sciences
Materials Science
Dermatology

Background:

Supersaturation is a known enhancer of fentanyl transport across silicone membranes using propylene glycol:water (PG:H2O) formulations.
Understanding drug behavior in human skin is crucial for effective transdermal delivery systems.

Purpose of the Study:

To evaluate supersaturated fentanyl formulations in human skin.
To screen polymers for stabilizing supersaturated formulations.
To assess permeation for both infinite and finite doses.

Main Methods:

Formulations with varying degrees of drug saturation (DS) were tested in human skin.
Hydroxypropylcellulose (HPC) was used to stabilize a 3 DS formulation.
Permeation studies were conducted for infinite and finite doses.
Tape-stripping experiments analyzed drug concentration in the stratum corneum.

Main Results:

Skin permeation increased linearly with drug saturation (DS) in infinite dose studies.
Silicone and skin flux values showed excellent correlation for infinite dose studies.
Fentanyl concentration in the stratum corneum was proportional to DS.
Drug crystallization due to solvent depletion affected finite dose studies.

Conclusions:

Supersaturation effectively enhances fentanyl permeation in human skin for infinite doses.
Vehicle stability is critical to maintain supersaturation and prevent crystallization for effective transdermal delivery.
Further research is needed to optimize vehicles for sustained drug release in finite dose transdermal systems.