Novel Application of Hot Melt Extrusion Technology for Preparation and Evaluation of Valacyclovir Hydrochloride Ocular Inserts.
Administration, Ophthalmic
Antiviral Agents
/ administration & dosage
Biological Availability
Calorimetry, Differential Scanning
Drug Compounding
/ methods
Drug Implants
Drug Liberation
Hot Melt Extrusion Technology
Keratitis, Herpetic
/ drug therapy
Polymers
/ chemistry
Valacyclovir
/ administration & dosage
acyclovir
antiviral
hot-melt extrusion
ocular drug delivery
ocular inserts
Journal
AAPS PharmSciTech
ISSN: 1530-9932
Titre abrégé: AAPS PharmSciTech
Pays: United States
ID NLM: 100960111
Informations de publication
Date de publication:
14 Jan 2021
14 Jan 2021
Historique:
received:
27
08
2020
accepted:
21
12
2020
entrez:
15
1
2021
pubmed:
16
1
2021
medline:
20
2
2021
Statut:
epublish
Résumé
The objective of this study was to investigate the processability of hot-melt extrusion (HME) to formulate ocular inserts of valacyclovir hydrochloride and evaluate the in vivo bioavailability of the formulation. To optimize the formulation of this drug, different physical mixtures of the polymers and plasticizer were prepared. The physical mixture was extruded through a co-rotating twin-screw extruder, and the obtained ocular inserts were cut with dimensions of 4 mm × 2 mm × 1 mm to enhance the formulation instillation in the eye. Ocular inserts were evaluated for drug content, weight variation, uniformity of thickness, in vitro drug release, and in vivo drug bioavailability. The ocular inserts were thermally characterized using differential scanning calorimetry (DSC). The attributes observed for the ocular inserts were within the target specifications. The ocular inserts of valacyclovir hydrochloride were successfully prepared using the HME. They provided sustained drug release along with enhanced drug permeation when compared with the eyedrop solution and dissolve completely in 8 h. Additionally, the obtained results demonstrated that the formulation of ocular inserts of valacyclovir hydrochloride using HME was reproducible, robust, and effective method.
Identifiants
pubmed: 33447869
doi: 10.1208/s12249-020-01916-5
pii: 10.1208/s12249-020-01916-5
pmc: PMC7886274
mid: NIHMS1665296
doi:
Substances chimiques
Antiviral Agents
0
Drug Implants
0
Polymers
0
Valacyclovir
MZ1IW7Q79D
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
48Subventions
Organisme : NIGMS NIH HHS
ID : P20 GM104932
Pays : United States
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