Open Access Short Research Article

Cytotoxic Effect of Lingzhi Extracts on Gefitinib-resitant Lung Cancer Cells

Nguyen Hai Dang, Pham Thanh Binh, Nguyen Thi Tham, Bui Thi Mai Anh, Nguyen Phuong Dai Nguyen, Nguyen Tien Dat

Journal of Pharmaceutical Research International, Page 1-5
DOI: 10.9734/BJPR/2016/23005

Aims: The present study was carried out to investigate the cytotoxicity of extracts from Ganoderma and Amauroderma lingzhi species collected in Tay Nguyen, Vietnam.

Methods: Mushroom samples were extracted by methanol and the cytotoxicity was performed by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide (MTT) method.

Results: Among twelve extracts prepared from Ganoderma and Amauroderma species, six samples significantly inhibited the proliferation of gefitinib-resistant NSCLC cell lines NCI-H1975 and A549. Amauroderma rugosum exhibited cytotoxic effects against both cell lines in comparison with etoposide.

Conclusion: The obtained results suggested that the Tay Nguyen lingzhi could be regarded as a promising candidate for natural sources of epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs).

Open Access Original Research Article

In vitro Antioxidant Activity and Hypolipidemic Effects of an Ethanol Extract of Amaranthus viridis Leaves on Hyperlipidemic Wistar Albino Rats

O. D. Omodamiro, M. A. Jimoh, P. U. Ezurike

Journal of Pharmaceutical Research International, Page 1-12
DOI: 10.9734/BJPR/2016/22124

Amaranthus viridis Linn. (AV), communally known as ‘Slender or Green Amaranth’ in English, is a multinational genus of herbs. Several species of Amaranthus are often considered as weeds, as leaf vegetables, cereals and ornamentals. Traditionally, an infusion of the plant (leaves and roots) is used to treat dysentery and epilepsy in children, purify blood, reduce inflammation, hemorrhoids, reduce labour pain and improve appetite in parts of Africa and India. The present study was designed to evaluate the In vitro antioxidant activity and hypolipidemic effect of an ethanol extract of AV leaves (EEAVL) in Wistar albino rats and mice using experimental models. Acute toxicity (LD50) of EEAVL were studied in mice using standard method. The result showed a LD50 of 353.6 mg/kg of the extract. Fourteen (14) Wistar albino rats of both sexes were divided randomly into seven (7) groups of two animals, each subjected to different treatment for 14 days. Group A was the non-high fat diet control; Group B was the high fat diet-induced control; Group C received 20 mg/kg of Simvastatin, a standard lipid lowering drug; Group D to G received 250 mg/kg, 125 mg/kg, 62.25 mg/kg and 31.13 mg/kg BW respectively of EEAVL of which all were still maintained on their induced diet. At the end of the treatment, the lipid profile and body weight were estimated and compared with the Simvastatin treated control group. The result showed a significant (p< 0.05) decrease in T-Cholesterol, Triglyceride and LDL-C (p> 0.05) while HDL-C was increased at the doses studied. EEAVL also caused a decrease in the rate of weight gain. In the in-vitro antioxidant test, there was a concentration dependent increase in the (%) Scavenging activity when compared with the Vitamin C (control) for 1,1-diphenyl-2-picrylhydrazyl (DPPH), Nitric oxide and anti-lipid peroxidation activity of AVL. The results showed no significant difference at higher concentrations when compared to the control. On a comparative basis, the measure of the antioxidant effectiveness of the extract showed better activity in quenching Nitric oxide radical with an IC50 values of 72 mg/ml compared to Lipid peroxidation radicals (78mg/ml) and DPPH radicals (108 mg/ml). The result have shown that Amaranthus viridis L, a traditional folklore medicinal plant has in vitro antioxidant potentials and hypolipidemic effect which may provide therapeutic potentials in the management of Cardiovascular diseases, diabetes and their complications which might be caused by free radical generation and hyperlipidemia.

Open Access Original Research Article

Formulation and Evaluation of Dexibuprofen Transdermal Films in Rabbits

Boushra Mohamed El-Houssieny, Esmat Zein El-Dein, Hussien Mohamed El-Messiry

Journal of Pharmaceutical Research International, Page 1-13
DOI: 10.9734/BJPR/2016/18988

Dexibuprofen is a practically water-insoluble nonsterodial anti-inflammatory drug. Following previous experience on enhancing the solubility of the drug, a mixed hydrotropic solubilization technique was here applied in order to improve the aqueous solubility of the drug so that a soluble form of dexibuprofen was prepared and then could be used as a main active ingredient in transdermal films. Nine formulae were prepared applying 32 full factorial design using different amounts of hydroxypropylmethylcellulose (HPMC) and polyvinylpyrrolidone K30 (PVP K30). The prepared formulae were evaluated for their physical properties, loading efficacy and In-vitro dissolution studies adopting the USP XXII dissolution method type V paddle over disk apparatus method. Permeation studies were done for best three films showing higher dissolution rate using Franz cell apparatus and also bioavailability study was carried out on the best formula to compare the absorption of dexibuprofen from the prepared film (treatment A) to commercial tablets (treatment B) following administration of a single dose to rabbits. The prepared films were off-white color, opaque, smooth, moist and non-sticky. Increasing the amounts of HPMC and PVP K30 lead to increasing weight, folding endurance, tensile strength, moisture content and moisture absorption. Transdermal films containing higher concentrations of PVP K30 and lower concentration of HPMC showed higher rate and amount of dexibuprofen released from dissolution medium and Franz cell. The bioavailability study showed that (Tmax) in treatments A and B is 3 hours and 2 hours respectively. The average peak plasma concentration values (Cmax) were 28.98±3.36 and 34.67±0.61 ug/mL, respectively and the AUC0-∞ values were 145.82±13.09 and 117.44±3.15 µg·h/mL, respectively. There were significant differences between treatments A and B in Cmax, t(1/2)ab,  Kel, t(1/2)el, TCR, AUC0-8, AUC0-∞, AUMC0-8, AUMC0-∞, and MRT. While the difference was insignificant in Kab.

Open Access Original Research Article

Fenofibrate Potentiates the Antihyperglycemic, Antidyslipidemic and Hepatoprotective Activity of Pioglitazone in Alloxan-Induced Diabetic Rats

Md. Tanjir Islam, Md. Shahid Sarwar, A. F. M. Towheedur Rahman, Md. Asaduzzaman, Yusuf Ali, Shaheda Zannah, Mamunur Rashid

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/22664

Aim: The present research was designed to investigate the hypoglycemic, hypolipidemic and hepatoprotective activity of the fixed dose combination of pioglitazone and fenofibrate.

Methodology: For the study purpose, pioglitazone at a dose of 15 mg/70 kg body weight (BW) and fenofibrate at a dose of 72.5 mg/70 kg BW were administered on alloxan (120 mg/kg BW) induced diabetic rats. Both the drugs (pioglitazone and fenofibrate), singly and in combination, separately were tested in vivo for 14 days (two weeks) to determine blood glucose level, lipid profile and hepatoprotective activity using Long-Evans male rats as test animals. In addition, to investigate any possible side effects of the combined therapy, the survival rate of rats were also measured.

Results: The study showed that in alloxan induced diabetic rats, combination therapy significantly decreased the blood glucose level from 16.00±0.01 to 7.85±0.03 mmol/L two hours later of last dose administration in comparison to the diabetic control group, after daily treatment for two weeks. In case of dyslipidemic effect, combination therapy reduced total cholesterol level by 31%, triglyceride level by 46% and LDL-cholesterol level by 37% significantly and increased HDL-cholesterol level by 77% in comparison with their respective diabetic control groups. It was also observed that combination therapy decreased alanine transaminase (ALT) level by 53% and aspartate transaminase (AST) level by 40% in comparison to diabetic control group effectively. These changes were significantly better than those of pioglitazone and fenofibrate monotherapy. No rats were died after combined treatment while the survival rates were 80%, 80% and 60% for pioglitazone, fenofibrate and diabetic groups (alloxan induced) respectively.

Conclusions: Our study suggests that the combination of pioglitazone and fenofibrate might be efficacious in patients with diabetic dyslipidemia and might provide better hepatoprotective activity in these patients.

Open Access Original Research Article

Preparation and Characterization of sPLGA Complex Microspheres as a Promising Carrier for Cucurbitacin B

Yi Zhang, Yue Liu, Hewei Shao, Xiaoyan Han

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/BJPR/2016/22575

The purpose of this research was to develop a new kind of GA-CS/sPLGA complexed Microspheres delivery system for CuB. In this work, star-shaped poly(lactic-co-glycolic acid) (sPLGA-COOH) and chitosan modified with glycyrrhetic acid (GA-CS) were successfully synthesized. The GA-CS/sPLGA complexed Microspheres for CuB was prepared by emulsion evaporation method. Futhermore, CuB-loaded Microspheres formulations were optimized. The release behaviour of CuB-loaded Microspheres in vitro were also examined. It was showed that CuB-loaded amount of Microspheres could reach 58.78%±1.288 by adding GA-CS into the external water phase. The size of corresponding CuB-loaded Microspheres was 370±16.14 nm in diameter, and zeta potential was negative 10.86±0.4790 mV measured by laser light particle size/zeta potential analysis. The results indicated that the complexed GA-CS/sPLGA Microspheres raised the entrapment efficiency for CuB. In vitro drug release demonstrated that complexed GA-CS/sPLGA Microspheres had many advantages such as sustained release and low initial drug burst.

Open Access Original Research Article

Molecular Detection of Mycobacterium tuberculosis Complex by GenoType®MTBDRplus from Patients Attending Bingham University Teaching Hospital, Jos, Nigeria

Chisom Olachi Ukaegbu, Agatha Ani, Agwu Ulu Nnachi

Journal of Pharmaceutical Research International, Page 1-11
DOI: 10.9734/BJPR/2016/22991

Aims: The study was to investigate the presence of M. tuberculosis and the resistance to rifampicin and isoniazid in AFB-positive sputa of patients attending Bingham University Teaching Hospital, Jos, Nigeria.

Study Design:  This was a prospective cross-sectional laboratory-based observational study.

Place and Duration of Study: The study was carried out in Bingham University Teaching Hospital (BUTH), Jos North, Plateau state, Northern Nigeria from April, 2013 to December 2013.

Methodology: A total of 90 AFB positive samples were collected from BUTH, Jos, and further screened for Mycobacterium tuberculosis using HAINS GenoType®MTBDRplus (HAIN Lifescience, Nehren, Germany).

Results: Eighty three (92%) out of the 90 AFB smear positive samples were positive for M. tuberculosis by GenoType®MTBDRplus line probe assay while the remaining seven (8%) were negative. Mycobacterium tuberculosis resistance to either or both RIF and INH were detected in 46/83 (55%) total cases; with RIF 24%, INH 17% and multidrug resistance (Resistance to both INH and RIF) 14%. The commonly observed mutation types in this research were rpoB MUT2B and inhA MUT1 for RIF and INH respectively.

Conclusion: The performance of GenoType®MTBDRplus to detect M. tuberculosis was excellent and the resistance detected was high in this region. Also, the overall level of resistance is noteworthy and suggestive of adverse public health implications with risk of increasing infection rates, on-going transmission, delayed therapy, increased mortality as well as development of secondary resistance known as extensively drug-resistant tuberculosis (XDR-TB). Prompt case detection and treatment strategy should be strictly adhered and to do this, rapid case detection molecular techniques such as HAINS GenoType®MTBDRplus is recommended.

Open Access Original Research Article

Effectiveness of Systemic Administration of Amoxycillin and Metronidazole versus Azithromycin in Generalized Aggressive Periodontitis – A Randomized Controlled Clinical Trial

Archana Mootha, Sankari Malaiappan, Sheeja S. Varghese, N. D. Jayakumar

Journal of Pharmaceutical Research International, Page 1-6
DOI: 10.9734/BJPR/2016/22732

Aim: To evaluate the effect of systemic Amoxycillin and Metronidazole against Azithromycin as an adjunct to non-surgical therapy and correlate the clinical periodontal parameters at baseline, 10 days and 30 days in subjects with generalized aggressive periodontitis (GAP).

Study Design: Randomized controlled clinical trial.

Place and Duration of the Study: The study was conducted in Saveetha Dental College and Hospitals from February 2015 to August 2015.

Methods: Subjects were recruited from the outpatient department of Periodontics and were categorized as GAP according to AAP criteria. A total of 16 patients with GAP were included in the study. Clinical periodontal parameters like sulcus bleeding index [SBI], gingival index [GI], Probing depth [PD] and clinical attachment loss [CAL] were recorded at baseline. The subjects were then randomly allotted into Group 1 [Amoxycillin+Metronidazole] and Group II [Azithromycin]. After evaluation of clinical parameters at baseline, scaling and root planning [SRP] was done in both the Groups and systemic antibiotics, namely combination of Amoxycillin and Metronidazole in Group I and Azithromycin in Group II were administered. Subjects were recalled at day 10 and 30 for re-evaluation of clinical parameters. Within Group comparison was made using paired “t test” and inter Group comparison was made using Un-paired “t test”. 

Results: Intra-Group comparisons of clinical parameters between baseline and 30 days, in both the Groups were statistically significant (P<0.05). The difference from baseline to 30 days follow up in sulcus bleeding index (8.7±0.59 versus 4.1±0.38 mm) and clinical attachment loss (8.8±0.48 versus 4.6±0.39 mm) was statistically significant between the Groups (P<0.05). Whereas no statistical significance was found with gingival index and probing depth between the Groups (P>0.05).

Conclusion: Systemic administration of Azithromycin as an adjunct to SRP in subjects with GAP resulted in better improvement of clinical periodontal parameters compared to a combination of Amoxycillin and Metronidazole.