Author: Ishraq Kadhim Abbas

AbstractA third of recently created drugs have poor water solubility and absorption. Innovative methods, such as self-nanoemulsifying drug delivery systems (SNEDDS), are being developed to address issues with pharmaceutical delivery and bioavailability.These systems, which are referred to as isotropic mixtures, are made up of the drug, a suitable oil, a surfactant, and either a co-surfactant or co-solvent. These elements combine to create a “oil in water (O/W)” nanoemulsion after being lightly stirred.Colloidal systems, including microemulsions and nanoemulsions, are being used more commonly in food, cosmetics, and pharmaceutical preparations to encapsulate, protect, and transport lipophilic components. The nanoscale particles used in these kinds of delivery systems have several potential benefits, including enhanced long-term stability, enhanced solubility, enhanced optical transparency, and enhanced bioavailability. To create SNEDDS, one can utilize a phase diagram technique statistical design of trials. For SNEDDS, switching from a liquid to a solid dose form may have improved stability as well as increased patient compliance. The design and production of SNEDDS and their effects on the bioavailability of several medications are the subject of numerous studies in this review. Keywords: Bioavailability, Solubility, Self-nano emulsifying drug delivery system, Oral bioavailability DOI: https://doi.org/10.54133/ajms.v3i.91

Overactive bladder (OAB) affects about 16% of adults and rises with increasing age. OAB lead to various symptoms such as urgency, incontinence, urinary frequency and nocturia. Darifenacin hydrobromide (DH) is the more recent uroselective M3 receptor antagonist for treating uncomplicated OAB. Fast-dissolving buccal films are the most innovative oral solid dosage form because of their flexibility and comfort. This study aims to formulate DH as fast-dissolving buccal films (FDBFs) using a solvent casting method to increase its bioavailability by reducing the effect of first-pass metabolism in the liver. Films were prepared by using polyvinyl alcohol as a film-forming polymer, glycerol and tween 80. Different types and concentrations of super disintegrants (croscarmellose sodium, sodium starch glycolate, indion 414) were used to select the best formula by studying the physicochemical properties of the films, disintegration time (DT) and percent drug release. The results revealed that formula (F9) that containing 7.5mg DH, 2%w/v PVA, 30%w/w glycerol, 0.5%w/v tween 80, 4%w/w indion 414 was the preferred formula. F9 showed the shortest in-vitro disintegration time (31.28sec). The in-vitro dissolution profile showed the lowest T80 %of the drug in 3.05 min and the highest release of the drug (94%) within 5 min (D5min %). It was concluded that the FDBFs of DH could be considered a promising drug delivery system with an enhanced disintegration and dissolution rate and better patient compliance. Keywords: Darifenacin hydrobromide, Overactive bladder, Fast-dissolving buccal films DOI:https://doi.org/10.31351/vol28iss2pp83-94

AbstractBackground: Supersaturable self-nanoemulsion (S-SNE) is an approach for dealing with low oral bioavailability problems. Bilastine (BL) is a selective H1-antihistamine with a bioavailability of 59%. Objective: To use a liquisolid technique to transform liquid BL S-SNE into powder so that both the S-SNE and liquisolid procedures could be used. Methods: Oleic acid, tween 60, transcutol, and soluplus were used to make the liquid BL-loaded S-SNE that was adsorbed onto the Avicel PH101 and Aerosil 200 admixtures. In vitro dissolving and powder flow characteristics were tested. SEM, DSC, X-ray diffraction, FT-IR analysis, and the average droplet size after dispersion in 0.1N HCl were also utilized to define the best formula’s solid state. Results: The best liquid-solid composition, SS-F2, is composed of oleic acid, tween 60, transcutol, soluplus, Avicel 101, and Aerosil 200, with a liquid SNE to Avicel 101 ratio of 1.5:1 and an Avicel 200 to Aerosil 200 ratio of 10:1. SS-F2 displayed good flowability and a significant improvement in drug dissolution, with 100% of the medication released after 60 min compared to 62.27% of the marketed BL tablets. According to the solid-state investigation of formula (SS-F2), BL was shown to be in a solvated state in the solidified nanosystem, with no interactions with the excipient used. It also formed a nanoemulsion with mean droplet sizes of 77.57 nm and a PDI of 0.4178, which was similar to liquid S-SNE. Conclusion: The liquisolid technique is a potential method for solidifying a liquid self-emulsifying system while preserving self-nanoemulsion characteristics and increasing dissolving rate. Keywords: Liquisolid powder, Bilastine, SNEDDS, Dissolution efficiency DOI: https://doi.org/10.54133/ajms.v5i.160

Self-nanoemulsifying drug delivery systems are innovative methods that have a potential to resolve a variety of drug formulation issues, including solubility, stability and bioavailability. Bilastine is a potent and high selective H1-antihistamine. The aimof this study is to develop bilastine as an oral self-nanoemulsion to enhance its permeability and possibility of lymphatic transport. Based on the solubility investigations of bilastine in some oils, surfactants and cosurfactants, fifteen formulas of liquid self-nanoemulsion drug delivery systems (SNEDDS) were formulated utilizing oleic acid, tween 60 and transcutol as oil, surfactant and co-surfactant respectively. Pseudoternary phase diagrams were used to evaluate the component phase behavior and the area of the nanoemulsion. The prepared formulas were evaluated for particle size, polydispersity index, zeta-potential, self-emulsification time, drug content, and robustness to dilution. When compared to the pure drug powder, the produced SNEDDS formulations showed enhanced drug release. This study showed that a formula 8 with a 20% oleic acid, 40% tween 60, and 40% transcutol composition exhibited lower particle size (71.976 ± 0.23 nm)and higher zeta-potential (-20.32) with acceptable drug content (95 %± 0.42) compared to other formulas and better in-vitro drug release characteristics than pure bilastine powder. All of these criteria favor the development of self-nano emulsifying drug delivery systems as a potential approach to enhance the bioavailability of drugs like bilastine that are poorly soluble.Keywords: Antihistaminic drug, Bilastine, SNEDDS, Transcutol, Tween 60 .Introduction Bilastine (BL) is a new, well tolerated second generation H1-antihistamine. It is indicated for the treatment of chronic spontaneous urticaria and seasonal rhino conjunctivitis (1). BL is also effective in all nasal symptoms including obstruction and in allergic conjunctivitis (2). It belongs to BCS class II (3). Its chemical formula is C28H37N3O3 and its Mwt is 463.61 Dalton, Log Pis 2.41(4). Its bioavailability is about 60%(5). Self-nanoemulsifying drugdelivery systems(SNEDDS)are lipid-based formulations that, when in contact with the aqueous medium of gastrointestinasecretionswhile being lightly stirred by peristaltic activity, generate a small oil-in-water nanoemulsion (6). The drug is presented in solubilized state in this spontaneous emulsion, and the droplets small size creates a significant amount of interfacial area on the surface for absorbing drug (7). These factors together lead to enhance bioavailability. 1Corresponding author E-mail:ishraqalmualla@yahoo.comReceived: 28/4 /2023Accepted: 22/ 6 /2023Iraqi Journal of Pharmaceutical Sciences DOI link: https://doi.org/10.31351/vol32issSuppl.pp164-176