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pH-swelling chitosan–xanthan gels that hold acyclovir

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Free-radical chitosan/xanthan/AMPS networks barely swell in acid but open in intestine-like pH, trapping up to 90.64% acyclovir.

Source

Chitosan/Xanthan Gum Based Hydrogels as Potential Carrier for an Antiviral Drug: Fabrication, Characterization, and Safety Evaluation

Malik NS, Ahmad M, Minhas MU, et al. · Frontiers in chemistry · 2020

doi.org/10.3389/fchem.2020.00050Read the full paper ↗75 citationscc by

Study at a glance

Design
Other — Chitosan–xanthan–AMPS hydrogels for acyclovir loading, swelling, and pH-dependent release
N
Formulation study of hydrogel batches (e.g., FCX6/FCX8) — no subject N
Population
Acyclovir-loaded chitosan/xanthan graft hydrogels in SGF/SIF media
Outcome
Drug entrapment efficiency and 24 h release at pH 1.2 vs 7.4

Structured fields used in claim comparison tables when every cited study has a complete layer.

What they did

Authors graft-polymerized chitosan and xanthan with AMPS/MBA/KPS, confirmed the network by FTIR and porous SEM, measured swelling in SGF (pH 1.2) vs SIF (pH 7.4), and loaded 1% acyclovir to get %DEE and 24 h release.

What they found

Optimized FCX6: 90.64% entrapment and 87.57% release at pH 7.4; FCX8 minimum DEE 76.83%. Swelling rises with CS 4→8 g, XG 1→3 g, AMPS 15→35 g; extra MBA or too much KPS cuts swelling. Release is low at pH 1.2 and high at 7.4.

The limits

What it doesn't show

Human PK of the gel is not measured; acute oral toxicity in animals is a safety screen, not a clinical bioavailability trial.

Key terms

AMPS
2-Acrylamido-2-methylpropanesulfonic acid, a hydrophilic ionic monomer.
SGF vs SIF
Simulated gastric (pH 1.2) vs intestinal (pH 7.4) fluids.
%DEE
Drug entrapment efficiency of acyclovir in the gel.
MBA crosslinker
N,N′-methylenebisacrylamide; more of it lowers swelling.
pH-responsive swelling
Network expansion when sulfonate/amine ionization increases at intestinal pH.

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FCX6 entrapment efficiency:

Common questions

Best %DEE?

FCX6 90.64%.

Where does it swell?

Much more in SIF pH 7.4 than SGF pH 1.2.

Optimal CS/XG?

8 g CS and 3 g XG.

How is the network made?

Free-radical polymerization.

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