Original Article

Studies on pH gradient loading of amphoteric drug (Doxorubicin hydrochloride) into liposome

Kishore K. Dondilkara^a,*, R.S.R. Murthy^b

^aDepartment of Pharmaceutical Research, Nobel Ilac A.S. San. Ve Tic. Duzce, Turkey.

^bM.S.R.University of Applied Sciences, MSR Nagar, Bangalore, India.

*Corresponding Author. Tel.: +91-7222968087, E-mail address: kishoredondilkar@gmail.com

The present study was carried out with an aim to evaluate the factors influencing the active drug loading through transmembrane pH gradient using Ammonium Sulphate. (AS) The influence of various factors which influence the pH gradient loading of amphoteric drugs [Doxorubicin Hydrochloride (DH) in our case] such as incubation temperature, incubation time, transmembrane migration of ammonium ions, molarity which influence the pH gradient loading of amphoteric drug were investigated. Initially, optimization of AS (100mM) loading into HSPC liposomes by thin film hydration method were done and later influence of incubation time (0.5, 1, 2 and 3 hours) and incubation temperature (RT, 40, 50 and 60°C) on DH were investigated. Incubation time of 3 hours and incubation temperature of 60°C was found to be optimum for maximum loading of DH. AS of different molarity (20 to 300Mm) were loaded into HSPC and its effect on drug loading was investigated. Increase in molarity brought about the increase in loading of DH and liposome formulation AS (225Mm) gave maximum loading. Measurement of internal pH prior and after drug loading could correlate the influence of all the above parameters on the loading of DH through pH gradient method. Besides, physiochemical characterization of developed liposomes, in-vitro drug release studies, in-vivo pharmacokinetics studies of the prepared liposomal formulation and the related stability studies were also carried out.

Keywords: pH Gradient, Ammonium Sulphate, Doxorubicin hydrochloride, Optimisation, Drug Loading

Original Article

Preliminary study on antioxidant and hepatoprotective activity of Clerodendrum phlomidis (L) against CCl4 intoxicated albino rats

Sapna A. Kondalkar^a, Avinash Kondalkar^b,*, A. K. Pathak^c

^aDepartment of Pharmacognosy, Truba Institute of Pharmacy, Bhopal, Madhya Pradesh, India.

^bDepartment of Pharmacognosy, NRI Institute of Pharmacy, Bhopal, Madhya Pradesh, India.

^cDepartment of Pharmacy, Barkatullah University, Bhopal, Madhya Pradesh, India.

*Corresponding Author. Tel.: +91 9926370524, E-mail address: kondalkar29@gmail.com

Ethanolic extract of leaves, root and stem of C. Phlomidis (Verbenaceae) were prepared by continuous hot percolation. The content of total flavonoid for each extract was determined by aluminium chloride colorimetric method and the percentage content of flavonoids were determined as quercetin equivalent. The potential of drug against free radicals is evaluated by in- vitro DPPH radical scavenging assay. Hepatoprotective activity was investigated on albino rats and carbon tetrachloride (CCl4 ) was used to produce hepato- toxicity. Ethanolic extract of leaves showed the maximum activity, which is comparable to the standard silymarin, while other parts were found to be less significant.

Keywords: Clerodandrum phlomidis, Hepatoprotective, Antioxidant, DPPH, Carbon tetrachloride (CCl4)

Original Article

Quantitative estimation of Eflornithine by Nitrite (Diazotization) titration

Amit Kumar^a,*, Vijender Singh^b, Praveen Kumar^c

^aTeerthankar Mahaveer University, (TMU), Teerthanker Mahaveer College of Pharmacy, Moradabad, Uttar Pradesh, India.

^bBBS Institute of Pharmaceutical & Allied Sciences, Greater Noida, India.

^cMoradabad Educational Trust Group of Institutions Faculty of Pharmacy, Moradabad, Uttar Pradesh, India.

*Corresponding Author. Tel.: +9897144639, E-mail address: amit81ak@gmail.com

Eflornithine hydrochloride (DFMO) being a primary aliphatic amine reacts with the nitrous acid (in situ liberation by the reaction of ice cold sodium nitrite and hydrochloric acid) and gets converted to diazonium salt. At the end point an excess drop of titrant sodium nitrite from the burette liberates nitrous acid; this free acid is determined by the starch-mucilage paper, used as an external indicator. The free nitrous acid reacts with potassium iodide and reduces the iodide to free iodine, which produces intense blue color with the alpha-amylose portion of the starch indicating the end point. The Eflornithine hydrochloride (DFMO, Difluoromethylornithine) determined by Diazotization Titration (DAT M-01). Here the amino group of Eflornithine is diazotized with sodium nitrite solution in cold acid solution. The nitrous acid formed diazotizes the compound. The iodine formed reacts with starch mucilage to give the blue color. The end point can be determined by using starch iodide paper as external indicator. The percentage of purity in DFMO is found 99.74%.

Keywords: Eflornithine hydrochloride, Nitrite Titration, Diazonium salt, Indicator, End point

Original Article

Wound healing activity reported on leaf extract of Murraya paniculata (Linn) on albino wistar rats

Sangeeta Gupta^a,*, Amit Singh^b

^aSchool of Pharmacy, Technocrates Group of Institution, Piplani, Anand nagar, Bhopal, Madhya Pradesh, India.

^bThe Pharmaceutical College, Samaleshwari Vihar, Barpali, Barghar, Orissa, India.

*Corresponding Author. Tel.: +91 9627953280, E-mail address: nicesangi@gmail.com

Murraya paniculata (L) (Family – Rutaceae) is an evergreen shrub or occasionally a small tree, known for its pharmacological activities like anti-inflammatory, antidiabetic and stimulant and analgesic and antioxidant properties etc. The present study was aimed to assess the wound healing potential of crude methanol extract and aqueous extract of Murraya paniculata (leaf) using three types of wound models in rats as incision wound, excision wound and dead space wound. The parameters studied include rate of wound contraction and period of epithilization, collagen content in excision wound model. Tensile strength, hydroxyproline estimation and granuloma tissue weight were studied in incision and dead space wound model and assessed alongwith histopathalogical examination. The treatment of wound with the methanol and aqueous extract was performed in graded dose manner. Higher dose of methanol extract (200 mg/kg b.w.) show significant effect by decreasing period of epithilization, increasing wound contraction rate, increase in tensile strenghth, hydroxyproline content and granulation tissue weight in the wounded rats and more effective when compared with aqueous extract and control. While aqueous extract (200 mg, 100 mg/kg b.w) show more significant effect than the control. Therefore, M. Paniculata leaves accelerated wound healing activity in rats and thus supports its traditional use.

Keywords: Murraya paniculata, Wound healing, Excision model, Incision model

Original Article

Development and validation of RP-HPLC method for the assay of Celecoxib capsule

Vaishalia^a,*, Vikas K. Singh^b

^aMoradabad Educational Trust, Group of Institutions, Faculty of Pharmacy, Moradabad, (U.P.) India.

^bTeva Pharma India, Plot No.189, Verna Industrial Estate, Verna, Goa, India.

*Corresponding Author. Tel.: +91 9456222750, E-mail address: vaishalihi009@gmail.com

Celecoxib is 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1yl] benzene1-sulfonamide. A simple and accurate reversed phase liquid chromatography method (HPLC) method was developed for the quantitative estimation of celecoxib, a selective COX-2 inhibitor in capsule formulations. The drug was chromatographed on a reversed-phase C-18 column. Eluents were monitored at a wavelength of 220 nm using a mixture (600:400:1:1) of acetonitrile, Water, Triethylamine and Orthophosphoric acid. The retention time of Celecoxib was found to be 9.5 minutes. The flow rate of the mobile phase was 1.0 ml/min at room temperature. The percentage recovery lies in the range of 99.53%–99.75%. Solution concentrations were measured on a weight basis to avoid the use of an internal standard. The method was statistically validated for linearity, accuracy, precision, selectivity and intermediate Precision. Due to its simplicity and accuracy, we believe that the method will be useful for routine quality control analysis. The method was validated as per ICH guidelines.

Keywords: Celecoxib, RP-HPLC, ICH guidelines, Validation

Original Article

Fabrication and characterization of Metformin loaded floating microspheres

Hitesh Kumar*, Ashok Kumar Rajpoot

Moradabad Educational Trust, Group of Institutions, Faculty of Pharmacy, Moradabad-244001, (U.P.), India.

*Corresponding Author. Tel.: +91 9917562680, E-mail address: hiteshmpharm@gmail.com

The aim of this study was to fabricate and characterize Metformin hydrochloride floating microspheres using Eudragit RS100 as a polymer. Microspheres were prepared by non-aqueous solvent evaporation method using ethanol/liquid paraffin system. The influence of formulation factors (drug: polymer ratio, stirring speed, concentration of surfactant) on particle size, encapsulation efficiency and in vitro release characteristics of the microspheres were investigated. The yields of preparation and encapsulation efficiencies were high for all formulations obtained. Mean particle size changed by changing the drug: polymer ratio or stirring speed. Although Metformin hydrochloride release rates from Eudragit RS100 microspheres were decreased as the concentration of Eudragit RS100 increased. By applying one way ANOVA followed by Newman-Keuls Multiple Comparison value obtained (p< 0.05) was considered to be statistically significant.

Keywords: Metformin hydrochloride, Eudragit RS100, Floating microspheres

Original Article

Synthesis and Evaluation of Substituted 1, 3, 4-Thiadiazole as Potential Antimicrobial Agent

Anuj Singhai^a,b,*, Shankar Kumar^b, Rajeev Saxena^c, Anindya Goswami^c, Hemant Nagar^c

^aDepartment of Pharmaceutical Chemistry, Truba Institute of Pharmacy, Bhopal, Madhya Pradesh, India.

^bDepartment of Pharmaceutical Chemistry, K.L.E.U’s College of Pharmacy, Vidyanagar, Hubli, Karnataka, India.

^cTruba Institute of Pharmacy, Bhopal, Madhya Pradesh, India.

*Corresponding Author. Tel.: +91 9424454220, E-mail address: anujsinghai1989@gmail.com

New series of N-(substituted phenyl)-2-[(5-substituted)-1,3,4-thiazol-2-yl)]acetamide (IVa-l) were synthesized by condensation of N-(substituted phenyl)-2-(5- sulfanyl-1,3,4-thiadiazol-2-yl) acetamide (IIIa-d) with different 2° amines. The structure of the synthesized compounds were characterized on the basis of physiochemical and spectral analysis (IR, and 1H-NMR). All these newly synthesized compounds (IVa-l) were screened for their antimicrobial and antifungal activity. The compounds IVc, IVf, IVg, IVj, IVl showed the good antibacterial activity and IVc and IVj showed the moderate antifungal activity.

Keywords: Thiadiazole, 1,3,4-Thiadiazole, Antimicrobial, Antifungal

Original Article

Synthesis, anticonvulsant (Chemo shock) activity of Isatin Mannich bases of quinazolone derivative

Meena K Yadav^a,*, Laxmi Tripathi^b

^aDepartment of Pharmaceutical Sciences, Saroj Institute of Technology and Management, Lucknow, Uttar Pradesh, India.

^bMoradabad Educational Trust Group of Institutions Faculty of Pharmacy, Moradabad, Uttar Pradesh, India.

*Corresponding Author. Tel.: +91 9838485610, E-mail address: meenayadav82@gmail.com

New N-methyl isatin [N-methyl -3-aryl -3H-quinazoline-4-one] derivatives 4(a-d) were synthesized and screened for anticonvulsant activity by strychnine, isoniazid (INH) and thiosemicarbazide induced chemo shock convulsion models. The neurotoxicity of the compounds was found by rotarod test. All the compounds were reported moderate protection of mice at 30 mg/kg at 0.5- 2 hr. in the entire test. No neurotoxicity was observed at the highest dose of 300 mg/kg for all the compounds.

Keywords: Isatin, Quinazoline, Strychnine, INH, Thiosemicarbazide, Mannich reaction

Review Article

Nutraceuticals

Ujjwal K. Singh, Swati N. Deshmukh*

Alard College of Pharmacy, Marunji, Pune, Maharashtra, India.

*Corresponding Author. Tel.: +91 8888797543, E-mail address: swatindeshmukh@rediffmail.com

In recent years there is a growing interest in nutraceuticals which provide health benefits and are alternative to modern medicine. Nutraceutical-rich vegetables and fruits are an important component of a healthy diet. It has been shown that people consuming healthy diets, living active lifestyles, not smoking and not indulging in excessive alcohol consumption tend to have a reduced risk of CVD. There has been an explosion of consumer interest in the health enhancing role of physiologically-active specific nutraceuticals. Such products include food supplements, dietary supplements, value-added processed foods as well as non-food supplements such as tablets, soft gels, capsules etc. The explosive growth, research developments, lack of standards, marketing zeal, quality assurance and regulation will play a vital role in its success or failure.

Keywords: Macronutrients, Micronutrients, Nutraceutical, Prebiotics, Probiotics

Original Article

Comparative wound healing activity of different marketed formulation in albino wistar rats

Maneesh Soni *, Jagdish Rathi, Pooja Malviya, Paridhi Thakur, Prity Singh, Rahul Rawat

Department of Pharmacology, NRI Institute of Pharmaceutical Sciences, Raisen Road, Bhopal, Madhya Pradesh, India.

*Corresponding Author. Tel.: +91 9977484175, E-mail address: manishsoni.pharmacist@gmail.com

The present study was aimed to compare in-vivo topical wound healing activity of different marketed formulation in wistar rats by excision and incision wound models. Three different marketed formulations were chosen to have different formulae. The animals were grouped into; group I (left untreated) considered as control, group II (Povidone Iodine 5% w/w, once daily), Group III (Mupirocin 2% w/w, once daily), group IV (Povidone Iodine 5% w/w + Mupirocin 2% w/w in 1:1 ratio, once daily). The healing effect of the formulations was accessed as excision wound area measurement, Percentage wound contraction and epithelialization period in the excision wound model, however wound breaking strength was accessed in the incision wound model. The results of the present study revealed that, animals treated with Mupirocin 2% ointment shows significant wound healing potential in comparison to control and other treatment groups. Mupirocin showed a significant and faster rate of wound contraction (p<0.001) as compared with control with the minimum epithelialization period as compared to other groups. Mupirocin also showed significant tensile strength (p<0.001) as compared to control. So the study concludes that mupirocin might be a drug of choice for better healing. Such type of comparative study is also further can be done on a large scale to find out more better significant results.

Keywords: Wound, Contraction, Excision, Incision, Povidone, Mupirocin, Epithelization, Tensile