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Yousuf, Rabia Ismail (2)
Al Sabah Siddiqi, Saniah (1)
Attia, Ismail A. (1)
Baloğlu, Esra (1)
Bushra, Rabia (1)
Donia, Ahmed M. (1)
El-Gizawy, Sanaa A. (1)
Fouda, Medhat A. (1)
Ghorab, Mohamed Khalid (1)
Hanif, Muhammad (1)
Hashem, Fahima M. (1)
Hashmat, Durriya (1)
Hyusein, Ismail Yuksel (1)
Ismail, Aliaa (1)
Jabeen, Sabahat (1)
Karavana, Sinem Y. (1)
Köse, Timur (1)
Lakhani, Fahim (1)
Mehmood, Zafar Alam (1)
Nasr, Mohamed (1)
Rehana, Saeed (1)
Shaker, Dalia S. (1)
Shoaib, M. Harris (1)
Shoaib, Muhammad Harris (1)
Zaheer, Kamran (1)
Year of Publication
Formulation, Characterization, and Clinical Evaluation of Microemulsion Containing Clotrimazole for Topical Delivery
Hashem, Fahima M.
Shaker, Dalia S.
Ghorab, Mohamed Khalid
The objective of the present study was to formulate and evaluate microemulsion systems for topical delivery of clotrimazole (CTM). The solubility of CTM in various oils was determined to select the oil phase of the microemulsion systems. Pseudoternary phase diagrams were constructed to identify the area of microemulsion existence. Five CTM microemulsion formulations (M1–M5) were prepared and evaluated for their thermodynamic stability, pH, refractive index, droplet size, viscosity, and in vitro release across cellulose membrane. Among the prepared microemulsion formulations, M3 (lemon oil/Tween 80/n-butanol/water) and M4 (isopropyl myristate/Tween 80/n-butanol/water) microemulsion systems were found to be promising according to their physical properties and CTM cumulative percentage release. Gel form of M3 and M4 were prepared using 1% Carbopol 940 as the hydrogel matrix. Both formulations were evaluated in the liquid and gel forms for drug retention in the skin in comparison to the marketed CTM topical cream and their stability examined after storage at 40°C for 6 months. Microemulsion formulations achieved significantly higher skin retention for CTM over the CTM cream. Stability studies showed that M4 preparations were more stable than M3. The in vitro anti-fungal activity of M4 against Candida albicans was higher than that of the conventional cream. Moreover, clinical evaluation proved the efficacy and tolerability of this preparation in the treatment of various topical fungal infections.
clotrimazole; microemulsion; skin retention; topical cream; topical gel
Development and Evaluation of Hydrophilic Colloid Matrix of Famotidine Tablets
Shoaib, Muhammad Harris
Al Sabah Siddiqi, Saniah
The objective of the present study was to develop a once-daily sustained-release (SR) matrix tablet of famotidine. Nine different formulations (F1–F9) were prepared by direct compression method using Avicel PH101 as filler/binder in the range of 41–27% in F1–F3, 18–22% in F4–F7, and 16–18% in F8–F9 and hydroxypropyl methylcellulose (4,000 cps) as hydrophilic matrix was used in F1–F3 from 19% to 30%, around 40% in F4–F7, and 42–45% in F8–F9. Talc and Aerosil were added in the ratio of 0.7–1.2%. The tablets were subjected to various physical parameters including weight variation test, hardness, thickness, diameter, friability, and in vitro release studies. Assay was also performed according to the USP 30 NF 25 procedure. The results of the physical parameters and assay were found to be within the acceptable range. In vitro dissolution results indicated that formulation F4–F7, having around 40% of rate control polymer, produced a SR pattern throughout 24 h. F1–F3 showed drug release at a faster rate, while F8–F9 released much slower, i.e., <80% in 24 h. Model-dependent and model-independent methods were used for data analysis and the best results were observed for F4 in zero order (r2 = 0.984) and F6 in Korsmeyer and Higuchi (r2 = 0.992 and 0.988). The parameter n indicated anomalous diffusion, while β in Weibull showed a parabolic curve with higher initial slope. The f2 similarity test was performed taking F4 as a reference formulation. Only the F5–F7 formulations were similar to the reference formulation F4. The mean dissolution time was around 10 h for the successful formulation.
famotidine; hydrophilic colloid matrix; hydroxypropyl methylcellulose (HPMC); kinetics; sustained release
Design and Formulation of Mebeverine HCl Semisolid Formulations for Intraorally Administration
Karavana, Sinem Y.
Gel formulations of mebeverine hydrochloride (MbHCl) containing hydroxypropylmethylcellulose (HPMC), metolose (MTL), and poloxamer 407 (PLX) were prepared to be used in the treatment of different oral painful conditions. HPMC was used as a mucoadhesive gel base while MTL and PLX were used to prepare sol–gel thermosensitive gels. MTL and PLX formulations showed proper sol–gel transition temperature for intraoral application. Formulations were evaluated in terms of their viscosity, mechanical properties, mucoadhesivity, stability, and in vitro drug release. The formulation prepared with 2% of HPMC K100M provided the highest viscosity at room temperature. However, the viscosity of HPMC–PLX mixture showed a significant increase at body temperature. The greatest mucoadhesion was also noted in HPMC–PLX combinations. Texture profile analysis exhibited the differences of the adhesion, hardness, elasticity, cohesiveness, and compressibility of the formulations. The release profiles of MbHCl were obtained, and non-Fickian release was observed from all the formulations. The formulations were stored at different temperature and relative humidity. No significant changes were observed at the end of the 3 months. HPMC–PLX formulation of MbHCl was chosen for in vivo studies, and it remained longer than dye solution on the rabbit’s intraoral mucosal tissue. It was found worthy of further clinical evaluation.
hydroxypropylmethylcellulose; mebeverine hydrochloride; mucoadhesion; poloxamer 407; sol–gel transition
Development of Enteric Coated Flurbiprofen Tablets using Opadry/acryl-eze System—A Technical Note
Shoaib, M. Harris
Mehmood, Zafar Alam
acryl-Eze; direct compression; enteric coating; flurbiprofen; opadry
Influence of a niosomal formulation on the oral bioavailability of acyclovir in rabbits
El-Gizawy, Sanaa A.
Fouda, Medhat A.
Donia, Ahmed M.
The purpose of this research was to prepare acyclovir niosomes in a trial to improve its poor and variable oral bioavailability. The nonionic surfactant vesicles were prepared by the conventional thin film hydration method. The lipid mixture consisted of cholesterol, span 60, and dicetyl phosphate in the molar ratio of 65:60:5, respectively. The percentage entrapment was ∼11% of acyclovir used in the hydration process. The vesicles have an average size of 0.95 µm, a most probable size of 0.8 µm, and a size range of 0.4 to 2.2 µm. Most of the niosomes have unilamellar spherical shape. In vitro drug release profile was found to follow Higuchi’s equation for free and niosomal drug. The niosomal formulation exhibited significantly retarded release compared with free drug. The in vivo study revealed that the niosomal dispersion significantly improved the oral bioavailability of acyclovir in rabbits after a single oral dose of 40 mg kg−1. The average relative bioavailability of the drug from the niosomal dispersion in relation to the free solution was 2.55 indicating more than 2-fold increase in drug bioavailability. The niosomal dispersion showed significant increase in the mean residence time (MRT) of acyclovir reflecting sustained release characteristics. In conclusion, the niosomal formulation could be a promising delivery system for acyclovir with improved oral bioavailability and prolonged drug release profiles.
Acyclovir niosomes; oral acyclovir; bioavailability of acyclovir
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