Hypertension shows circadian blood pressure rhythms (day-night pattern) that urge the delivery of antihypertensive drugs at the right time in the desired levels. Thus, a bilayered core-in-cup buccoadhesive tablet was formulated that immediately releases olmesartan, to give a burst effect, and controls azelnidipine release, to prolong its therapeutic effect. The main challenge was the poor bioavailability of azelnidipine due to its poor aqueous solubility and first-pass effect. Hence, liquisolid compact buccoadhesive tablets were prepared to enhance solubility, dissolution profiles, and bypass the oral route. Two factorial designs were conducted to study the type and concentration effect of the mucoadhesive polymers on the dissolution and mucoadhesion of olmesartan and azelnidipine. Characterization studies were conducted regarding drug content, surface pH, water uptake, mucoadhesive strength, in vitro release, and ex vivo permeability. The core-in-cup olmesartan/azelnidipine buccoadhesive tablet showed similar release profile to the statistically optimized formulae of each drug. In vitro dissolution study showed enhanced release of azelnidipine than the directly compressed tablets, to comply with the regulatory standards of controlled release systems. In vivo pharmacokinetic study of olmesartan and azelnidipine conducted on human volunteers against Rezaltas® 10/8 mg tablet showed percentage relative bioavailability of 106.12 and 470.82%, respectively.
Reduced bioavailability of azelnidipine is related to its poor aqueous solubility and extensive first-pass metabolism, which hinder its efficacy. These problems were addressed by implementing (1) a liquisol technique for promoting the dissolution rate in a controlled-release manner and (2) a core-in-cup bucco-adhesive drug delivery system as an alternative to the oral route. A 33 factorial design was used to study the effects of polymer type (sodium carboxymethyl cellulose (CMC Na), chitosan, or Carbomer P940) concentration (5, 10 or 15 %) and preparation technique (simple mix, liquisol or wet granulation) on the dissolution and mucoadhesion of core-in-cup azelnidipine buccoadhesive tablets. Tablet micromeritics, swelling index, mucoadhesive strength and in vitro release were characterized. Statistical analyses of these factors show ed significant effects on the studied responses, where F#16 prepared by the liquisol technique and containing 15 % CMC Na was chosen with an overall desirability of 0.953.
Hair dyes have been used to cover gray hair or to give an appealing look. In the present study, the extract of Calendula Officinalis was used in preparing a hair dye. This represents a natural gateway in development of hair dye to avoid damage caused by synthetic dyes. The yellow coloring principle of the extract, Calendulin, was converted into nano-sized formula ensuring hair fiber penetration. Nine formulae were prepared by solvent evaporation technique, based on a 32 factorial design using Design Expert® program, independent variables being: speed and time of homogenization; three levels: low, medium and high. Polyvinyl alcohol (0.5% w/v) was used as stabilizing agent. Formulae were evaluated by determination of Zeta size, potential and polydispersity index. Response surface modeling enabled choosing the optimal formula (least particle size, polydispersity index and highest zeta potential), which was evaluated by transmission electron microscopy and dyeing effect as a gel containing 0.5% Carboxymethyl cellulose. F7, produced by operating the homogenizer at 26000rpm for 10 minutes proved to be optimal which succeeded to dye white hair and lighten up the black hair as evidenced by optical microscope images. Hence it was recommended to use F7 in covering the white hair.
With its simplicity and cost–effectiveness, the liquisolid technique offers solutions for numerous formulation problems. Among these are dissolution enhancement and sustaining drug release, and the liquisolid technique dealt with both approaches. This review focuses on the latest advances in the technique. It discusses modified additives for use as carrier materials, which secure the required large surface area for enclosing liquids. The review also covers the modern liquipellet technique derived from the extrusion/palletization technique. Also, the liquiground term is introduced, combining the advantages of co-grinding with the liquisolid concept. Furthermore, several grades of Eudragits, and hydrophilic retarding polymers are mentioned to explain modes of sustaining drug release. This review sums up the liquisolid technique development and its applications recently achieved.
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