Related Experiment Video
Updated: Mar 28, 2026
09:51
Microfluidic Production of Lysolipid-Containing Temperature-Sensitive Liposomes
Published on: March 3, 2020
10.0K
Novel Controlled Release Polymer-Lipid Formulations Processed by Hot Melt Extrusion
Mohammed Maniruzzaman1, Muhammad T Islam1, Sheelagh Halsey2
1School of Sciences, Faculty of Engineering and Science, University of Greenwich, Chatham Maritime, Kent, ME4 4TB, UK.
AAPS Pharmscitech
|December 23, 2015
Summary
Novel polymer/lipid formulations enhanced indomethacin (INM) dissolution rates. Hot melt extrusion (HME) created amorphous solid dispersions with synergistic effects observed in vitro.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Indomethacin (INM) is a water-insoluble non-steroidal anti-inflammatory drug (NSAID).
- Improving the dissolution rate of poorly soluble drugs is crucial for enhancing bioavailability.
Purpose of the Study:
- To investigate the impact of novel polymer/lipid solid dispersions on indomethacin dissolution.
- To explore the synergistic effects of hydroxypropyl methyl cellulose polymer (HPMCAS) and stearoyl macrogol-32 glycerides-Gelucire 50/13 (GLC) on drug release.
Main Methods:
- Hot melt extrusion (HME) using a twin-screw extruder to produce solid dispersions.
- Characterization techniques including X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and hot stage microscopy (HSM).
- In-line monitoring using near-infrared (NIR) spectroscopy and in vitro dissolution studies.
Main Results:
- Characterization confirmed the presence of amorphous indomethacin within the HPMCAS/GLC matrices.
- NIR spectroscopy indicated drug-polymer/lipid interactions and hydrogen bonding.
- In vitro studies revealed a 2-hour lag time in acidic media, followed by significantly enhanced indomethacin dissolution at pH > 5.5.
Conclusions:
- Novel polymer/lipid formulations processed by HME effectively create amorphous solid dispersions of indomethacin.
- The HPMCAS/GLC carrier system exhibits a synergistic effect, enhancing indomethacin dissolution rates under specific pH conditions.
Related Concept Videos
01:19Modified-Release Drug Delivery Systems: Rate-Programmed II
89
Rate-programmed drug delivery systems release drugs in a controlled manner to maintain therapeutic levels. Three main designs include reservoir, matrix, and hybrid systems.Reservoir systems consist of a drug core enclosed within a membrane that controls drug release. In non-swelling reservoir systems, polymers like ethyl cellulose or polymethacrylates are used. These do not hydrate in aqueous media and control release through membrane thickness, porosity, or insolubility. This type includes...
89
01:22Modified-Release Drug Delivery Systems: Rate-Programmed I
102
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,...
102
01:23Modified-Release Drug Delivery Systems: Classification
250
Modified-release drug delivery systems improve drug efficacy and minimize side effects by controlling the rate and location of drug release. These systems fall into three categories: rate-programmed, stimuli-activated, and site-targeted.Rate-programmed systems release drugs at a predetermined rate, maintaining consistent therapeutic levels and reducing fluctuations that could lead to toxicity or subtherapeutic effects. These systems use polymeric matrices, reservoir-based designs, or osmotic...
250
01:30Modified-Release Drug Delivery Systems: Stimuli-Activated
115
Stimuli-activated drug delivery systems are designed to release drugs in response to specific physical, chemical, or biological stimuli. These systems often utilize hydrogels—three-dimensional, hydrophilic polymer networks capable of swelling in aqueous environments and retaining significant fluid volumes. Upon exposure to particular stimuli, these hydrogels undergo structural transitions that allow the embedded drug to be released. Due to this adaptive behavior, such systems are also...
115
01:20Modified-Release Drug Delivery Systems: Influencing Factors
128
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...
128
01:24Site-Targeted Drug Delivery Systems: Polymeric Carriers
109
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...
109