Polymer-Free Injectable In Situ Forming Nanovesicles as a New Platform for Controlled Parenteral Drug Delivery Systems
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ORIGINAL ARTICLE
Polymer-Free Injectable In Situ Forming Nanovesicles as a New Platform for Controlled Parenteral Drug Delivery Systems Hussein O. Ammar 1 & Magdy Ibrahim 2 & Azza A. Mahmoud 1 & Rehab N. Shamma 2
&
Nada M. El Hoffy 1
Accepted: 19 October 2020 # Springer Science+Business Media, LLC, part of Springer Nature 2020
Abstract Purpose In this study, the preparation of self-assembled polymer-free in situ forming nanovesicles (ISNs) based on non-ionic surfactants (NISs) is presented. Methods A 22·41 full factorial experimental design was adopted for the development of novel polymer-free ISNs loaded with tenoxicam utilizing the emulsion method. The type of NIS (Brij® 52 or Span® 60), the cholesterol percentage (30, 50, or 60 w/w%), and the internal phase percentage (20 or 30 v/v%) were chosen as the independent variables. Percentage drug released after 1 h (Q1), vesicle particle size (PS), and mean dissolution time (MDT) were the dependent variables. Selected formulation was investigated morphologically using transmission electron microscopy. Results Results revealed that the formation had spherical dense shape. All independent factors significantly affected the percentage drug release after the first hour (Q1), and the MDT, while only the type of NIS had a significant effect on PS. The highest control of drug release was observed in formulation containing Span® 60 with lower internal phase percentage (MDT = 20.06 ± 0.40 h) as well as the smallest PS (123.75 ± 16.68 nm). Conclusion The obtained results indicated the potentiality of the invented ISNs in controlling the release of tenoxicam in a desirable economical biphasic pattern compared to other in situ formulations. Keywords In situ forming nanovesicles . Non-ionic surfactants . Ethyl acetate . Cholesterol . Tenoxicam
Introduction Parenteral sustained release drug delivery systems have been extensively investigated as they offer several advantages
* Rehab N. Shamma [email protected] Hussein O. Ammar [email protected] Magdy Ibrahim [email protected] Azza A. Mahmoud [email protected] Nada M. El Hoffy [email protected] 1
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University in Egypt, Cairo, Egypt
2
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt
over other systems. They are capable of reducing dosing frequency owing to the controlled drug release up to several months, thus better patient compliance, in addition to reducing fluctuations in drug level in plasma. Moreover, they are capable of providing improved bioavailability and localized high drug level [1, 2]. Several parenteral sustained release delivery systems have been introduced, such as solutions, emulsions [3], liposomes [4], micelles [5], implants [6], microparticles [7], nanoparticles, and nanocapsules [8]. Parenteral sustained release suspensions suffer from several problems, being a dispersed heteroge
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