Non-ionic Surfactant Based In Situ Forming Vesicles as Controlled Parenteral Delivery Systems

Non-ionic surfactant (NIS) based in situ forming vesicles (ISVs) present an affordable alternative to the traditional systems for the parenteral control of drug release. In this work, NIS based ISVs encapsulating tenoxicam were prepared using the emulsion method. Tenoxicam-loaded ISVs were prepared...

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Bibliographic Details
Published in:AAPS PharmSciTech 2018-04, Vol.19 (3), p.1001-1010
Main Authors: Ammar, Hussein O., Ibrahim, Magdy, Mahmoud, Azza A., Shamma, Rehab N., El Hoffy, Nada M.
Format: Article
Language:English
Subjects:
Animals
Biochemistry
Biomedical and Life Sciences
Biomedicine
Biotechnology
Delayed-Action Preparations
Drug Carriers - chemistry
Drug Liberation
Emulsions
Male
Particle Size
Pharmacology/Toxicology
Pharmacy
Piroxicam - administration & dosage
Piroxicam - analogs & derivatives
Polysorbates
Rabbits
Research Article
Surface-Active Agents - chemistry
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Summary:Non-ionic surfactant (NIS) based in situ forming vesicles (ISVs) present an affordable alternative to the traditional systems for the parenteral control of drug release. In this work, NIS based ISVs encapsulating tenoxicam were prepared using the emulsion method. Tenoxicam-loaded ISVs were prepared using a 2 2 .3 1 full factorial experimental design, where three factors were evaluated as independent variables; type of NIS (A), molar ratio of NIS to Tween®80 (B), and phase ratio of the internal ethyl acetate to the external Captex® oil phase (C). Percentage drug released after 1 h, particle size of the obtained vesicles and mean dissolution time were chosen as the dependent variables. Selected formulation was subjected to morphological investigation, injectability, viscosity measurements, and solid state characterization. Optimum formulation showed spherical nano-vesicles in the size of 379.08 nm with an initial drug release of 37.32% in the first hour followed by a sustained drug release pattern for 6 days. DSC analysis of the optimized formulation confirmed the presence of the drug in an amorphous form with the nano-vesicles. Biological evaluation of the selected formulation was performed on New Zealand rabbits by IM injection. The prepared ISVs exhibited a 45- and 28-fold larger AUC and MRT values, respectively, compared to those of the drug suspension. The obtained findings boost the use of ISVs for the treatment of many chronic inflammatory conditions.
ISSN:1530-9932
1530-9932
DOI:10.1208/s12249-017-0897-8