Showing papers by "Hibah M. Aldawsari published in 2015"

Design and formulation of a topical hydrogel integrating lemongrass-loaded nanosponges with an enhanced antifungal effect: in vitro/in vivo evaluation.

Abstract: Lemongrass oil (LGO) is a volatile oil extracted from the leaves of Cymbopogon citratus that has become one of the most important natural oils in the pharmaceutical industry because of its diverse pharmacologic and clinical effects However, LGO suffers from low aqueous solubility, which could lead to a reduced effect Moreover, the instability of its major active constituent, citral, could lead to volatilization, reaction with other formulation ingredients, and consequently, skin irritation To surmount these problems, this research aims to formulate lemongrass-loaded ethyl cellulose nanosponges with a topical hydrogel with an enhanced antifungal effect and decreased irritation The minimal inhibitory concentration and minimal fungicidal concentration of LGO against Candida albicans strain ATC 100231, determined using the broth macrodilution method, were found to be 2 and 8 μL/mL, respectively The emulsion solvent evaporation technique was used for the preparation of the nanosponges The nanosponge dispersions were then integrated into carbopol hydrogels (04%) Nine formulations were prepared based on a 32 full factorial design employing the ethyl cellulose:polyvinyl alcohol ratio and stirring rate as independent variables The prepared formulations were evaluated for particle size, citral content, and in vitro release Results revealed that all the nanosponge dispersions were nanosized, with satisfactory citral content and sustained release profiles Statistical analysis revealed that both ethyl cellulose:polyvinyl alcohol ratio and stirring rate have significant effects on particle size and percentage released after 6 hours; however, the effect of the stirring rate was more prominent on both responses The selected hydrogel formulation, F9, was subjected to surface morphological investigations, using scanning and transmission electron microscopy, where results showed that the nanosponges possess a spherical uniform shape with a spongy structure, the integrity of which was not affected by integration into the hydrogel Furthermore, the selected formulation, F9, was tested for skin irritation and antifungal activity against C albicans, where results confirmed the nonirritancy and the effective antifungal activity of the prepared hydrogel

Enhanced permeation parameters of optimized nanostructured simvastatin transdermal films: ex vivo and in vivo evaluation

Abstract: Objective: Detailed optimization process was carried out to enhance permeation parameters, and hence bioavailability, of simvastatin (SMV) transdermal films.Methods: SMV solubility was investigated in various oils, surfactants and co-surfactants/co-solvents. Mixtures of the selected components were prepared to identify zone of nanoemulsion formation that was utilized in Extreme Vertices mixture design to develop SMV self-nanoemulsifying drug delivery systems (SNEDDS) with minimum globule size. Optimized SMV-SNEDDS were included in the preparation of transdermal films. A fractional factorial design was implemented to evaluate effects of the factors on the amount of SMV permeated. The optimized film was investigated for ex vivo skin permeation and in vivo pharmacokinetic parameters.Results: The optimum SNEDDS formula was 0.09, 0.8 and 0.11 for Sefsol 218, tween 80 and PEG 200, respectively. Fractional factorial design depicted the optimized SMV transdermal film with 2% HPMC and 2% DMSO as permeation...

Innovation of natural essential oil-loaded Orabase for local treatment of oral candidiasis

Abstract: Purpose Oral candidiasis may be manifested in the oral cavity as either mild or severe oral fungal infection. This infection results from the overgrowth of Candida species normally existing in the oral cavity in minute amounts based on many predisposing factors. Several aspects have spurred the search for new strategies in the treatment of oral candidiasis, among which are the limited numbers of new antifungal drugs developed in recent years. Previous studies have shown that thyme and clove oils have antimycotic activities and have suggested their incorporation into pharmaceutical preparations. This study aimed to investigate the possibility of the incorporation and characterization of essential oils or their extracted active ingredients in Orabase formulations.

Gastroretentive Ranitidine Hydrochloride Tablets with Combined Floating and Bioadhesive Properties: Factorial Design Analysis, In Vitro Evaluation and In Vivo Abdominal X-Ray Imaging.

Abstract: Ranitidine HCl is an H2-antagonist that suffers from low oral bioavailability of 50%. The site-specific absorption from the upper part of the small intestine and the colonic metabolism of the drug could partially contribute to its reduced bioavailability. To surmount these drawbacks, this work aimed at the formulation of Ranitidine HCl gastroretentive floating-biaodhesive tablets. A 3(2) factorial design was applied to assess the effects of matrix former (HPMC K100M): drug ratio, and the release retardant (Carbopol 971) amount on the characteristics of the tablets prepared using direct compression technique. The prepared tablets were thoroughly evaluated for physical properties, floating, swelling, bioadhesive and in vitro release behaviors. Statistical analysis of the results revealed significant effects for both formulation variables on the swelling index, maximum detachment force and cumulative percent drug released after 6 hours. In addition, the matrix- former: drug ratio showed a statistically significant effect on the floating lag time. Kinetic analysis of the release data indicated Higuchi diffusion kinetics and anomalous transport mechanism for all formulations. Scanning electron micrographs of the selected tablet formulation; F8, revealed intact surface without any perforations or channels in the dry state, while polymer expansion (relaxation) with some perforated areas were observed on the surface of the tablets after 12 hours dissolution in 0.1 N HCl. Furthermore, in vivo abdominal x-ray imaging showed good floating behavior of the selected formulation; F8, for up to 6 hours with appropriate bioadhesive property. In conclusion, the selected ranitidine HCl floating-bioadhesive tablets could be regarded as a promising gastroretentive drug delivery system that could deliver the drug at a controlled rate.

Avanafil Liposomes as Transdermal Drug Delivery for Erectile Dysfunction Treatment: Preparation, Characterization, and In vitro, Ex vivo and In vivo Studies

Abstract: Purpose : To formulate avanafil, a recently approved phosphodiesterase-5 enzyme inhibitor, in liposomal form for enhanced transdermal permeation and bioavailability Methods : Two preparation procedures were employed, leading to the formation of multilamellar vesicles (MLVs) and reverse-phase evaporation unilamellar vesicles (ULVs). The effects of the preparation method and lipid content on the encapsulation efficiency and particle size were studied. Studies assessing the stability, in vitro release, ex vivo permeation and in vivo bioavailability were also conducted in rats. Results : The preparation of avanafil liposomes as MLVs, the addition of cholesterol, and the use of more rigid phospholipids all increased the avanafil encapsulation efficiency within the liposomes (95.61 %). The stability studies revealed that the liposomes prepared using phospholipids with higher transition temperatures (dipalmitoyl-L-α-phospatidylcholine) were significantly more stable for a longer period of time after storage at 25 ± 0.5 ˚C and 60 ± 5 % relative humidity for a period of 2 months (p < 0.05). In vivo pharmacokinetic results from rats showed a significant increase in the bioavailability of avanafil from transdermal liposomal formulations of up to 7-fold (p < 0.05) compared to the topical drug suspension. Conclusion : The developed avanafil liposomes represent a promising transdermal drug delivery system for the treatment of erectile dysfunction. Keywords : Avanafil, Liposomes, Entrapment efficiency, Dipalmitoyl-L-α- hospatidylcholine, Erectile dysfunction

Ultrasound effects on brain-targeting mannosylated liposomes: in vitro and blood–brain barrier transport investigations

Abstract: Delivering drugs to intracerebral regions can be accomplished by improving the capacity of transport through blood-brain barrier. Using sertraline as model drug for brain targeting, the current study aimed at modifying its liposomal vesicles with mannopyranoside. Box-Behnken design was employed to statistically optimize the ultrasound parameters, namely ultrasound amplitude, time, and temperature, for maximum mannosylation capacity, sertraline entrapment, and surface charge while minimizing vesicular size. Moreover, in vitro blood-brain barrier transport model was established to assess the transendothelial capacity of the optimized mannosylated vesicles. Results showed a dependence of vesicular size, mannosylation capacity, and sertraline entrapment on cavitation and bubble implosion events that were related to ultrasound power amplitude, temperature. However, short ultrasound duration was required to achieve >90% mannosylation with nanosized vesicles (<200 nm) of narrow size distribution. Optimized ultrasound parameters of 65°C, 27%, and 59 seconds for ultrasound temperature, amplitude, and time were elucidated to produce 81.1%, 46.6 nm, and 77.6% sertraline entrapment, vesicular size, and mannosylation capacity, respectively. Moreover, the transendothelial ability was significantly increased by 2.5-fold by mannosylation through binding with glucose transporters. Hence, mannosylated liposomes processed by ultrasound could be a promising approach for manufacturing and scale-up of brain-targeting liposomes.

Quality control assessment of locally manufactured aspirin tablets in comparison to globally produced generics

Abstract: Challenges confronting the locally manufactured medications in Saudi Arabia have been increasing in the last decade. The Saudi market is mainly built on imported medications. Meanwhile, local manufacturers are much neglected in the Saudi's market. Building consumer's trust for local medication is one of the main targets to achieve success in decreasing the rate of importing medication while increasing locally produced ones. This study aims to compare the quality of some of the marketed low dose enteric coated Aspirin tablets (as a model product) produced by local Saudi pharmaceutical companies (F1 and F3) with others manufactured by an Arabian Emirate company (F5), and two other brands of USA companies (F2 and F4) as global generics. F2 represents the proprietary product produced by Bayer (Bayer Aspirin ® ), to which all other brands were compared. Different quality control tests adopted by the United States Pharmacopeia and/or the British Pharmacopeia were applied to the five brands. Tablets were also assessed for physical and organoleptic properties. Results revealed that nearly all of the tested tablets met the requirements of the quality control tests adopted. This reflects their equivalency both pharmaceutically and statistically.