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

Abstract

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 2.3 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.

Celecoxib Loaded In-Situ Provesicular Powder and Its In-Vitro Cytotoxic Effect for Cancer Therapy: Fabrication, Characterization, Optimization and Pharmacokinetic Evaluation

“…The dialysis bag was then placed into 20 mL phosphate-buffered pH 7.4 containing 1% (w/v) sodium lauryl sulfate (SLS), acting as the receptor compartment, with the temperature maintained at 37 ± 0.5 • C in an incubation shaking water bath (WSB-18, Daihan Scientific Co. Ltd., Gangwon, South Korea) and shaked at 50 rpm. Samples were withdrawn at 1, 2, 3, 4, 5, 6, 7, 8, 12, 18 and 24 h time intervals, replaced with fresh buffer to keep the sink condition and then analyzed spectrophotometrically at 256 nm [10,27,28].…”

“…Vesicular systems such as liposomes and niosomes are the most common carriers used in order to entrap the drug molecules [9]. Regrettably, these vesicular systems have some drawbacks such as limited encapsulation, stability, and scaling up obstacles, which provoke the need for evolving new vesicular systems that can overcome such problems [10]. Among the promising new vesicular systems are in-situ forming provesicular drug carriers, which are pro-nanovesicles consisting of dry free flowing powder coated with surfactant, which can be hydrated just before use resulting in the formation of the nanovesicles facilitating the absorption of the incorporated drugs [11,12].…”

Statistical optimization of bile salt deployed nanovesicles as a potential platform for oral delivery of piperine: accentuated antiviral and anti-inflammatory activity in MERS-CoV challenged mice

“…Liposomes and niosomes are conventionally used vesicles to sheath drugs. Woefully, their restricted encapsulation efficiency and limited stability, and scaling up problems, the requisite for evolving novel vesicular systems was aroused (Ammar et al, 2018a ). Bile salts (BS) encompassing vesicles or bilosomes have been developed as a modification for liposomes and niosomes which offer more stable vesicles by addition of BS to the lipid bilayers (Aburahma, 2014 ).…”

Design, Green Synthesis and Tailoring of Vitamin E TPGS Augmented Niosomal Nano-Carrier of Pyrazolopyrimidines as Potential Anti-Liver and Breast Cancer Agents with Accentuated Oral Bioavailability

“…For the accurate characterization of the percentage of 2a and 7 charged within the formulated TPGS-modified niosomal dispersion, accurately; 1 mL of either 2a - or 7 -loaded TPGS-modified niosomes (representing 2 mg of each drug) were dispersed with 5 mL distilled water and manually agitated for 2 min for dilution. The cooling centrifugation technique for one hour was manipulated to discriminate the unenclosed either 2a or 7 from 2a - or 7 -charged TPGS-modified niosome at 15,000 rpm and 4 °C (Beckman, Fullerton, Mississauga, ON, Canada) [ 54 ]. The sedimented vesicles were harvested and centrifuged again for 30 min after being rinsed twice with distilled water.…”

“…The manipulated technique was a dynamic laser scattering technique to determine the distribution size at 25 °C using a 45 mm focus lens and a beam length of 2.4 mm. The test was performed in triplicate [ 54 ].…”