Abstract:The current study aims to develop niosomal nanocarriers for intranasal delivery of dronedarone hydrochloride to ameliorate its limited bioavailability. Niosomes were prepared by ethanol injection method and optimized using 3² full factorial experimental design. Both Span® type (X1) and Span®: cholesterol ratio (X2) were set as independent variables. Vesicle size (Y1), polydispersity index (Y2), zeta potential (Y3), and entrapment efficiency (Y4) were set as responses. The optimal formula was further incorporat… Show more
“…A non-Fickian mechanism transport generally occurs with the glassy (vitreous) polymeric system having the glass transition temperature beyond the experimental temperature. In this situation, the mobility of polymer chains is insufficient to allow the penetration of water molecules into the system core [ 39 , 54 , 55 ]. Case II transport is a particular situation of non-Fickian transport where the solvent front is expanded at a relaxation-controlled steady rate.…”
Section: Resultsmentioning
confidence: 99%
“…For Super Case II transport, the solvent diffusion occurs at a faster rate, accelerating the solvent penetration. The tension generated during the movement of the gel–vitreous interface causes polymer breakage [ 39 , 55 ].…”
Diarylheptanoids (DAs) characterized by a 1,7-diphenylheptane structural skeleton are considered a novel class of phytoestrogens. The DAs available in Curcuma comosa Roxb. (C. comosa) extract demonstrated significant estrogenic activities both in vitro and in vivo. This study aimed to develop and comprehensively evaluate a mucoadhesive vaginal gel for the sustained release of DAs. Different mucoadhesive polymers as gelling agents were investigated. C. comosa ethanolic crude extract was used as a source of DAs. All C. comosa gels were light brown homogeneous with pH within 4.4–4.6. Their flow behaviors were pseudoplastic with a flow behavior index of 0.18–0.38. The viscosity at a low shear rate varied from 6.2 to 335.4 Pa·s. Their mechanical and extrudability properties were associated well with rheological properties. Polycarbophil (PCP):hydroxypropyl methylcellulose (HPMC) blends had a higher mucoadhesiveness to porcine vaginal mucosa than those of PCP-based or HPMC-based gels. All C. comosa gels exhibited a sustained, zero-order DA release pattern over 72 h. Korsmeyer and Peppas equation fitting indicated a non-Fickian, case II transport release mechanism. C. comosa gels had good physical and chemical stability under low-temperature storage for up to 12 months. PCP:HPMC-based mucoadhesive gels could be a proper delivery system for vaginal administration of DAs.
“…A non-Fickian mechanism transport generally occurs with the glassy (vitreous) polymeric system having the glass transition temperature beyond the experimental temperature. In this situation, the mobility of polymer chains is insufficient to allow the penetration of water molecules into the system core [ 39 , 54 , 55 ]. Case II transport is a particular situation of non-Fickian transport where the solvent front is expanded at a relaxation-controlled steady rate.…”
Section: Resultsmentioning
confidence: 99%
“…For Super Case II transport, the solvent diffusion occurs at a faster rate, accelerating the solvent penetration. The tension generated during the movement of the gel–vitreous interface causes polymer breakage [ 39 , 55 ].…”
Diarylheptanoids (DAs) characterized by a 1,7-diphenylheptane structural skeleton are considered a novel class of phytoestrogens. The DAs available in Curcuma comosa Roxb. (C. comosa) extract demonstrated significant estrogenic activities both in vitro and in vivo. This study aimed to develop and comprehensively evaluate a mucoadhesive vaginal gel for the sustained release of DAs. Different mucoadhesive polymers as gelling agents were investigated. C. comosa ethanolic crude extract was used as a source of DAs. All C. comosa gels were light brown homogeneous with pH within 4.4–4.6. Their flow behaviors were pseudoplastic with a flow behavior index of 0.18–0.38. The viscosity at a low shear rate varied from 6.2 to 335.4 Pa·s. Their mechanical and extrudability properties were associated well with rheological properties. Polycarbophil (PCP):hydroxypropyl methylcellulose (HPMC) blends had a higher mucoadhesiveness to porcine vaginal mucosa than those of PCP-based or HPMC-based gels. All C. comosa gels exhibited a sustained, zero-order DA release pattern over 72 h. Korsmeyer and Peppas equation fitting indicated a non-Fickian, case II transport release mechanism. C. comosa gels had good physical and chemical stability under low-temperature storage for up to 12 months. PCP:HPMC-based mucoadhesive gels could be a proper delivery system for vaginal administration of DAs.
“… 57 In contrast to a high-viscosity Newtonian fluid, the pseudoplastic criterion enables a sustained drug release and satisfactory gel distribution over the nasal surface. 121 , 122 Figure 5 Rheological profiles of in-situ gel formulations. ( A ) at 4 ◦ C, ( B ) at 25 ◦ C, and ( C ) at gelling temperature.…”
Purpose
Immunomodulatory and broad-spectrum antiviral activities have motivated the evaluation of curcumin for Coronavirus infection 2019 (COVID-19) management. Inadequate bioavailability is the main impediment to the therapeutic effects of oral Cur. This study aimed to develop an optimal curcumin transferosome-loaded thermosensitive in situ gel to improve its delivery to the lungs.
Methods
Transferosomes were developed by using 3
3
screening layouts. The phospholipid concentration as well as the concentration and type of surfactant were considered independent variables. The entrapment efficiency (EE%), size, surface charge, and polydispersity index (PDI) were regarded as dependent factors. A cold technique was employed to develop thermosensitive in-situ gels. Optimized transferosomes were loaded onto the selected gels. The produced gel was assessed based on shape attributes, ex vivo permeability enhancement, and the safety of the nasal mucosa. The in vitro cytotoxicity, antiviral cytopathic effect, and plaque assay (CV/CPE/Plaque activity), and in vivo performance were evaluated after intranasal administration in experimental rabbits.
Results
The optimized preparation displayed a particle size of 664.3 ± 69.3 nm, EE% of 82.8 ± 0.02%, ZP of −11.23 ± 2.5 mV, and PDI of 0.6 ± 0.03. The in vitro curcumin release from the optimized transferosomal gel was markedly improved compared with that of the free drug-loaded gel. An ex vivo permeation study revealed a significant improvement (2.58-fold) in drug permeability across nasal tissues of sheep. Histopathological screening confirmed the safety of these preparations. This formulation showed high antiviral activity against SARS-CoV-2 at reduced concentrations. High relative bioavailability (226.45%) was attained after the formula intranasally administered to rabbits compared to the free drug in-situ gel. The curcumin transferosome gel displayed a relatively high lung accumulation after intranasal administration.
Conclusion
This study provides a promising formulation for the antiviral treatment of COVID-19 patients, which can be evaluated further in preclinical and clinical studies.
“…Ion-triggered polymers in ISS technology find application in the development of delivery systems for use on mucosa with a wide range of ionic compositions of biological fluids. Therefore, one of the most commonly realized routes of administration of ion-triggered polymer-based systems is intranasal administration [ 1 , 2 , 3 ].…”
Section: Introductionmentioning
confidence: 99%
“…The high compatibility of ion-triggered polymers with most APIs, including immunobiological substances, determines the relevance of using ISS as adjuvants for intranasal vaccination [ 3 , 23 , 24 , 25 ]. The administration of immunobiological drugs through the nasal cavity using adjuvant delivery systems allows both local immunization and systemic immune responses to be achieved.…”
The rapid growth in the prevalence of infectious diseases requires timely action from drug developers. In recent years, the COVID-19 pandemic has demonstrated the unpreparedness of the population for such emergencies. The introduction of modern methods of Design of Experiments (DoE) is required to accelerate the process of drug development and bring a drug to market. The main objective of this study was to develop an ion-triggered in situ system for intranasal delivery of VLP using a Quality by Design approach. Based on a literature review and initial studies, the key QTPP, CQA, CPP, and CMA were identified to develop a novel delivery system for virus-like particles. As a result of the studies on the quality attributes of the developed delivery system, an ion-triggered in situ gel meeting all the specified parameters was obtained using the Quality by Design method.
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