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

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 Characterization of Novel Non-Ionic Surfactant Based Aceclofenac Gel as a Potential Drug Delivery System

Background: Aceclofenac is considered to the first line drug in the symptomatic treatment of rheumatoid arthritis, osteoartheritis and ankylosing spondylitis. The successful treatment of arthritis depend on the maintenance of effective drug concentration level in the body, for which a constant and uniform supply of drug is desired. The short biological half-life (about 4 hrs) and dosing frequency more than once a day as well as (70-80%) of dose is excreted by renal transport make aceclofenac an ideal candidate for formulation of niosomal gel. Methodology: The niosomal gel of aceclofenac in order to sustain the release of aceclofenac topically, decreases the side effect of GI disturbance by maintaining the concentration of the drug in the blood and decrease the renal excretion as well as frequency of dosing. Niosomal gel was prepared by coacervation phase separation method. Preformulation studies, structural analysis, in-vitro drug release study, mechanism of drug release kinetic and data analysis (zero order, first order and higuchi’s model), percentage entrapment efficiency and stability study were performed (n=3). Anti-Inflammatory study was performed for final optimized formulation. Result and conclusion: It is revealed from preformulation studies that materials obtained for study did not show any incompatibility. Particle size was determined in the range of 9.46±1.055 to 12.91±3.587μm by using an optical microscope with calibrated eyepiece micrometer. Scanning Electron Microscopy of niosomes was performed to observe surface morphology and percentage entrapment efficiency of niosomes were reported in the range of 63.49±0.265% to 78.55±0.425%. From release kinetic modelling, it was analysed that the drug was released from niosomes by a diffusion-controlled mechanism. Lastly, stability study of all formulations was done in two different temperature and anti inflammatory activity of final optimised formulation was compared with marketed formulation (Voveran Emulgel). Results shows that the aceclofenac Niosomal gel showed fair anti-inflammatory activity but it was not as good as the commercial product.

Formulation and in-vitro evaluation of niosomal gel of gatifloxacin

A novel drug delivery system provides the delivery of drugs at a required rate into the body during the period of treatment as directed by the body. Formulation and evaluation of Noisome containing gatifloxacin using different concentrations of the polymer for controlled release. Pre-formulation study confirms the purity of the drug and compatibility of the drug with excipients using FT-IR. Tween 80 was found significant with the experimental results. An extensive investigation is needed concerning the depth of penetration into the skin, determination of zeta potential, and confirmation of configuration of phospholipids in the lipid bilayer. A significant loss of entrapped drug was found at the end of three month period when liposomal dispersions were stored at high temperature i.e. 25±20C. All gels were found under pH range 7.0 to 7.4, Spreadability under the range 6.6 to 7.6 cm, % drug content 98 to 100%, the viscosity of gels 98 to 115cp, and % permeation found in rage 75 to 91%. Excellent % Permeation Gel formulation GF-4 was found 91%. The drug release at raised temperatures may be associated with the lipid degradation in the bilayers results in membrane packing defects them leaky.

Curcumin Niosomes Prepared from Proniosomal Gels: In Vitro Skin Permeability, Kinetic and In Vivo Studies

Curcumin is a poorly water-soluble drug that is used for the treatment of inflammations, tumors, wound healing antioxidant and other diseases. In the current manuscript, it is successfully formulated into proniosome gels. The proniosomes are readily hydrated into niosomal formulations using warm water. Proniosomes were prepared using nonionic surfactants (tween 80, span 60) either solely or in combinations with cholesterol. The produced niosomal formulations were homogenous in size with vesicular sizes >343 and <1800 nm. The encapsulation efficiency percentage “EE%” of curcumin in niosomal formulations was different according to niosomal composition. It increased up to 99.74% in formulations of tween 80/Chol of 200 μmole/mL lipid concentration. Span 60/chol niosomes showed decreased curcumin EE%. Niosomal formulations showed increased SSTF and PC with enhancement ratios of more than 20-fold compared with curcumin suspension form. Kinetically, niosomes fitted to the Korsemeyer-Peppas model with non-Fickian transport according to their calculated n-values where curcumin suspension form showed Korsemeyer-Peppas kinetics with Fickian transport. Niosomal formulations deposited higher curcumin amounts in the skin compared with the suspension form. The best niosomal formulation (F9) was used for niosomal gel and emulgel fabrication. Finally, the anti-inflammatory activity of curcumin in various formulations was evaluated using a rat hind paw edema method and the % of swelling was 17.5% following 24 h in group treated with curcumin niosomal emulgel. In conclusion, this study suggests that the developed niosomal emulgel could significantly enhance the anti-inflammatory effect of curcumin and be an efficient carrier for the transdermal delivery of the drug.