Gamma oryzanol niosomal gel for skin cancer: formulation and optimization using quality by design (QbD) approach

Abstract

Skin cancer is fifth most diagnosed disease in human population due to ultraviolet radiation (UV) exposure. Gamma oryzanol (OZ) is a natural antioxidant, and it also has skin anti-aging properties. OZ is naturally found in rice bran oil. The main aim of the present work was to optimize OZ niosomal formulation using quality by design approach including one variable at a time and full factorial design. Niosomes were prepared by solvent injection method and characterized for size, polydispersity index, drug entrapment, and transmission electron microscopy. The optimized batch obtained at X1 [drug to span 60 molar ratio (1:5)], X2 [volume of hydration (75 mL)], and X3 [stirring speed (2500 rpm)] to Y1 [average vesicle size (196.6 nm)] and Y2 [entrapment efficiency (78.31%)] as dependent variables. The optimized OZ noisomes were formulated by niosomal gel to provide improved physicochemical stability upon topical application against UV. The niosomal gel was characterized using pH meter, viscometer, Draize test for skin irritancy, ex vivo permeation studies, and stability studies. Ex vivo permeation studies of OZ niosomal gel not only showed fourfold higher permeation but also exhibited better drug retention in dermal layers of skin as compared to OZ gel. Quality Target Product Profile of OZ niosomal formulation was generated. Risk analysis of optimized OZ gel suggested most critical quality attributes (CQAs) and critical process parameters (CPPs) to be characterized as low risk. Thus, γ-oryzanol niosomal gel for topical use can serve as a promising prophylactic treatment in skin cancer, and the developed prototype formulation can be further extended to future newly discovered drugs with similar characteristics. Graphical abstract

Formulation and Evaluation of Azithromycin-Loaded Niosomal Gel: Optimization, In Vitro Studies, Rheological Characterization, and Cytotoxicity Study

“…The appearance of the niosomal gels was found to be translucent white in color. The pH of the gel was 6.56 ± 0.05, within the neutral normal range of pH for topical preparations, indicating that it can prevent any potential skin irritation. , …”

“…The pH of the gel was 6.56 ± 0.05, within the neutral normal range of pH for topical preparations, indicating that it can prevent any potential skin irritation. 44,45 3.8. Rheological Studies.…”

Statistical modeling, optimization and characterization of andrographolide loaded emulgel for its therapeutic application on skin cancer through enhancing its skin permeability

“…To know the andrographolide release pattern, in-vitro release data were fitted to different kinetic models like zero order, first order, and Higuchi and Korsmeyer-Peppas equations ( Shah et al, 2021 ).…”

Influence of Co-amorphization on the Physical Stability and Dissolution Performance of an Anthelmintic Drug Flubendazole

“…Various strategies have been developed to improve the bioavailability of small molecules, such as pharmaceutical salts, − cocrystals, pharmaceutical solvates, − gels, and compositions with polymers and cyclodextrins. − Several techniques have been proposed in the literature for improving the pharmaceutically relevant characteristics of FluBZ, including the use of ionic liquids, binary crystals, and nanoemulsions, as well as incorporation in cyclodextrin cavities. − Amorphization is one of the most commonly utilized methods for increasing the apparent solubility and permeability of an active pharmaceutical ingredient (API). , However, amorphous pharmaceuticals are thermodynamically unstable phases that tend to crystallize during manufacture, storage, and dissolution. , Development of a homogeneous single-phase co-amorphous system consisting of an API and a second component, on the other hand, efficiently suppresses crystallization, prolonging the shelf life of a product while keeping the benefits of the amorphous form . Furthermore, combining two synergistic APIs into a co-amorphous system may boost treatment efficiency, potentially leading to attractive fixed-dose combinations. , …”

“…Various strategies have been developed to improve the bioavailability of small molecules, such as pharmaceutical salts, 4−7 cocrystals, 8 pharmaceutical solvates, 9−11 gels, 12 and compositions with polymers and cyclodextrins. 13−16 Several techniques have been proposed in the literature for improving the pharmaceutically relevant characteristics of FluBZ, including the use of ionic liquids, binary crystals, and nanoemulsions, as well as incorporation in cyclodextrin cavities.…”