Open Access Original Research Article

Total Phenolics and Antioxidant Activity of Defatted Fresh Taif Rose, Saudi Arabia

El-Sayed S. Abdel-Hameed, Salih A. Bazaid, Mohamed M. Shohayeb

Journal of Pharmaceutical Research International, Page 129-140
DOI: 10.9734/BJPR/2012/1493

Recently, the residues or by-products of agriculture industry take attention for their valuable source of natural antioxidants. Taif rose (Rosa damascena trigintipetala Dieck) is considered one of the most important economic products of Taif, Saudi Arabia. In this study, the antioxidant and total phenolic contents of the defatted flowers of fresh Taif rose were investigated. The antioxidant activity was chemically determined using three methods; 1,1-diphenyl picrylhydrazyl (DPPH.) free radical scavenging activity, phosphomolybdenum method and reducing power activity. The methanol extract showed antiradical activity with SC50=49.44 mg/ml. Different fractions obtained from successive fractionation of the methanol extract with organic solvents of different polarities; chloroform (CHCl3), ethyl acetate (EtOAc) and n-butanol (n-BuOH); showed that, the EtOAc fraction had higher antiradical activity than n-BuOH fraction, and their respective SC50 were 15.62 and 36.29 mg/ml. On the other hand, CHCl3 fraction had a poor antiradical activity (SC50>100 mg/ml). The total phenolics, flavonoids, flavonols and RP-HPLC analysis of the methanol extract and its EtOAc and n-BuOH fractions were determined. The ethyl acetate fraction had the highest contents of phenolics, flavonoids and flavonols that correlated with the antioxidant activity. From this work, it is obvious that the by-product from concrete oil production of Taif rose could be used as a good inexpensive source of antioxidant polyphenolics.

Open Access Original Research Article

Formulation and Evaluation of Gel Forming Ocular Minitablets Containing Piroxicam

Abd EL–Gawad H. Abd EL–Gawad, Osama A. Soliman, Susan A. Barker, Germeen N.S. Girgis

Journal of Pharmaceutical Research International, Page 141-167
DOI: 10.9734/BJPR/2012/1653

Aims: The purpose of this in vitro and ex vivo study was to prepare and characterise ocular minitablets of piroxicam based on different polymeric matrices and to evaluate their potential to provide prolonged and controlled drug release to ocular tissues after surface administration.
Study Design: Experimental study and ex-vivo study.
Place and Duration of Study: School of Pharmacy, University of East Anglia, Norwich, Norfolk, UK, between July 2011 and March 2012.
Methodology: A range of placebo minitablet formulations were prepared based on pharmaceutically-acceptable polymers of differing chemical and physical properties. These were evaluated using standard physical and visual imaging methods. A subset of placebo formulations was chosen to prepare medicated minitablets containing 5 %w/w piroxicam as a model drug. Three different in vitro methodologies were used to assess drug release from the minitablets. An ex vivo porcine ocular method was used to assess likely tissue distribution of the drug after surface ocular administration of the minitablets.
Results: Minitablets were successfully produced from all formulations. The in vitro drug release profile was dependent on the chemistry of the polymer used, its hydration and swelling behaviour and to some extent, the methodology used for assessing the drug release profile. The ex vivo studies in porcine eyes suggested that the drug disposition was inversely related to the hydration and swelling behaviour of the polymer. Minitablets containing piroxicam based on Pluronic F127 showed the highest posterior segment ocular bioavailability of the formulations studied in the ex vivo model. Conversely, the more highly swelling minitablet formulations showed higher anterior segment bioavailability.
Conclusions: Ocular minitablets containing 5 %w/w piroxicam were successfully produced from a range of polymer matrices. In vitro release was shown to be dependent on the physical and chemical properties of the polymers used as the basis of the minitablets. Posterior segment deposition in an ex vivo model was greatest in the formulation which showed limited hydration and swelling behaviour in a simulated ocular environment.

Open Access Original Research Article

Piper sarmentosum Improves Bone Structure and Biomechanical Strength of Rats Given Excess Glucocorticoid

S. Ima Nirwana, M. R. Elvy Suhana, M. A. Siti Fadziyah, H. S. Farihah, A. Fairus, M. N. Muhamad Alfakri

Journal of Pharmaceutical Research International, Page 168-187
DOI: 10.9734/BJPR/2012/1435

Aims: To determine the effect of Piper sarmentosum (Ps) leaf extract on biomechanical strength and trabecular structure of the bones of glucocorticoid-induced osteoporotic rats.
Study Design: Administration of crude extract to rats with excessive glucocorticoids.
Place and Duration of Study: Department of Anatomy and Pharmacology, National University of Malaysia, between September 2010 and December 2011.
Methodology: Three-month old male Sprague-Dawley rats were adrenalectomized to remove the main source of circulating glucocorticoids. The animals were replaced with dexamethasone 120 µg/kg body weight/day. Treatment with P. sarmentosum 125 mg/kg body weight and glycirrhizic acid (GCA) 120 mg/kg body weight were given simultaneously for 2 months. After been sacrificed, a three-point bending configuration test for assessing the biomechanical properties of the right femoral bones was done using an Instron Universal testing machine equipped with Instron Bluehill software. The left undecalcified femoral bones were embedded in resin, sectioned and stained with Von Kossa for structural histomorphometric measurements.
Results: P. sarmentosum extract had significantly increased the intrinsic parameter (flexure modulus) and extrinsic parameter (energy at break) of the biomechanical properties of the bone. It had also significantly improved the trabecular structure by increasing the BV/TV, Tb.Th, Tb.N and by reducing the Tb.Sp based on histomorphometric analysis.
Conclusion: P. sarmentosum extract was able to protect bone biomechanical strength in glucocorticoid-induced osteoporotic bone, as confirmed by the structural histomorphometric finding. Therefore, Ps extract has the potential to be used as an agent to protect the bone strength and structure against osteoporosis due to chronic glucocorticoid treatment. These results however, need further study for better justification.

Open Access Original Research Article

Evaluation of Analgesic, Antidiarrhoeal and Cytotoxic Activities of Ethanolic Extract of Bacopa monnieri (L)

Hemayet Hossain, Md. Sariful Islam Howlader, Shubhra Kanti Dey, Arpona Hira, Arif Ahmed

Journal of Pharmaceutical Research International, Page 188-196
DOI: 10.9734/BJPR/2012/1951

Aims: The crude ethanolic leaf extract of Bacopa monnieri (L) Penn. (family: Scrophulariaceae) was evaluated for its possible phytochemical nature (group determination of plant constituent) and selected pharmacological activities (analgesic, antidiarrhoeal and cytotoxic activity) growing in Bangladesh.
Methodology: The antinociceptive activity was evaluated by acetic acid induced writhing model, antidiarrhoeal activity by castor oil induced diarrheal method and cytotoxicity by brine shrimp lethality bioassay.
Results: Phytochemical analysis of the ethanolic extract of B. monnieri indicated the presence of reducing sugar, tannins, steroid, alkaloid, saponin and gum types of compounds. The ethanolic extract of B. monnieri has effect on acetic acid induced writhing in mice. At the dose of 250 mg/kg and 500 mg/kg of body weight, the extract produced 36.69% and 59.17% writhing inhibition in test animals respectively. The results were statistically significant (p <0.01 and p <0.001) and was comparable to the standard drug Diclofenac Na, which showed 72.78% at a dose of 25 mg/kg weight. The ethanolic extract of B. monnieri has effect on castor oil induced diarrhea in mice. The result showed that the extract decreased the mean number of defecation which were 35.42 % and 47.92 % (p <0.001) at the doses of 250mg/kg and 500mg/kg respectively. The latent period for the extract treated group was increased (p <0.01) as compared to control group. The ethanolic of extract of B. monnieri showed significant toxicity to the brine shrimp nauplii. The concentrations of crude extract for 50% mortality (LC50) and 90% mortality (LC90) were 40 μg/mL and 150 μg/mL respectively.
Conclusion: Therefore, the obtained results tend to suggest the antinociceptive, antidiarrhoeal and cytotoxic activities of crude ethanolic extract of Bacopa monnieri leaves and thus provide the scientific basis for the traditional uses of this plant part as a remedy for pain and diarrhoea.

Open Access Original Research Article

To Explore the Ulceroprotective and Antioxidant Potential of Hyssopus officinalis in Ethanol-Induced Gastric Ulcers in Rats

Amita Saini, Ramica Sharma

Journal of Pharmaceutical Research International, Page 197-214
DOI: 10.9734/BJPR/2012/1930

Aim: To explore the ulceroprotective and antioxidant potential of Hyssopus officinalis in ethanol-induced gastric ulcer in rats.
Study Design: Administration of plant extract and evaluation of antiulcer activity.
Place and Duration of Study: Department of Pharmacology, Rayat Institute of Pharmacy, Railmajra, Distt. SBS Nagar. Performed between August 2011- June 2012.
Methodology: In the present study 1 ml of ethanol was administered to the overnight fasted rats which were sacrificed after 1 hour. Ethanolic extract of Hyssopus officinalis (EEHO) at the dose of 100 and 125 mg/kg was administered to albino rats 1 hour before the administration of ethanol. Animals were there then sacrificed and tissue homogenate was used for various biochemical parameters in order to explore the ulceroprotective and antioxidant potential of the plant.
Results: Administration of 1 ml of ethanol to overnight fasted rats resulted in increased ulcer index, total acidity and decreased pH. Further, it has been observed that in ethanol administered rats there was increased generation of reactive oxygen species estimated by increased level of TBARS and attenuated levels of glutathione, superoxide dismutase and nitric oxide along with decreased secretion of mucin. Further, ethanol administration too has a detrimental effect on the integrity of stomach. Pre-treatment with EEHO showed a great antiulcer and antioxidant potential depicted by decreased generation of ROS, improved the integrity of stomach, and increased the nitric oxide level. Most importantly, EEHO significantly improved the mucus secretion estimated by gastric adhesion mucus content.
Conclusion: The findings of the study indicate that pre-treatment with EEHO has a significant ulceroprotective and antioxidant activity in ethanol-induced ulcers, which supports its traditional use in folk medicine. This may open vista to explore various other therapeutic implications of this plant.