Development and characterization of biodegradable chitosan nanoparticles loaded with lovastatin using factorial design

The objective of the present work was to formulate chitosan nanoparticles as carriers for the lovastatin, since this drug undergoes extensive first pass extraction in the liver, and bioavailibity is low (< 5 %). Nanoparticles were prepared by modified ionotropic gelation method using 32 full factorial design. From the preliminary trials, the constraints for independent variables X1 (concentration of chitosan) and X2 (concentration of sodium tripolyphosphate) have been fixed and examined to investigate effect on particle size, encapsulation efficiency, zeta potential, % release, SEM, FTIR, XRD and DSC analysis of lovastatin. The diameter of prepared nanoparticles was controlled in the range of 100-800 nm, spherical shape and narrow diameter distribution. The release profiles of all batches were very well fitted by both the zero order model and the anomalous transport. These results indicate that lovastatin nanoparticles could be effective in sustaining drug release for a prolonged period.Colegio de Farmacéuticos de la Provincia de Buenos Aire

DESIGN AND DEVELOPMENT OF FLOATING PULSATILE DRUG DELIVERY OF LOSARTAN POTASSIUM

Objective: The objective of the present investigation was to the development of floating pulsatile drug delivery system of Losartan potassium (LP) tablets for obtaining no drug release during floating followed by pulsed, rapid drug release to achieve chronotherapeutic release. In hypertension, the risk of getting heart attacks early in the morning is high and therefore, there was need to develop drug delivery, which will release drugs at morning hours and provide efficacious therapy. LP is a short biological half-life (1.5-2.5h) and readily absorbed from the stomach and upper gastrointestinal tract. Methods: Tablet formulation was prepared by press coating of rapid release core tablets and core tablets were further top coated with a buoyant layer of HPMC K4M and sodium bicarbonate. Various grades of HPMC polymer (E5/E15/E50) were used for the pulsatile coating layer. The developed formulations were characterized for physical characteristics, floating lag time, floating time, release lag time, drug content, swelling index, in vitro dissolution studies, DSC and XRD. Results: The FTIR and DSC studies predicted that there was no chemical interaction between drug and excipients. The core tablet coated with HPMC E50 showed a high swelling index and release the drug 97.60±1.2% at 6h. Buoyant layer with 80 mg HPMC K4M and 25 mg sodium bicarbonate gave satisfactory floating lag time. Conclusion: The system showed an excellent lag phase followed by burst release in the distal small intestine, which gives site and time-specific delivery of LP acting as per chronotherapy for treatment of hypertension

Vacuum foam dried sugar-phosphate amorphous mixtures for stabilization of doxorubicin hydrochloride

The objective of the present study was to stabilize doxorubicin hydrochloride in sugar-phosphate amorphous mixtures at ambient temperature by drying it with vacuum foam drying. Finished products were evaluated for foam characteristic, residual moisture content, reconstitution time, percent drug recovery and drug-excipient interactions. FTIR studies revealed existence of physical interaction of drug with sugar. Light microscopy showed formation of amorphous glass which was supported by the observations of XRPD analyses. The optimized composition in vacuum foam drying was processed by lyophilization and their stability was compared. Storage at ambient temperature for 6 months showed that stability of vacuum foam dried product was better than lyophilized products. The amount of residual moisture affected the stability of drug. The detailed study revealed lactose and sodium dihydrogen phosphate is best suited for stabilization of doxorubicin hydrochloride at room temperature.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Research Journal of Pharmaceutical, Biological and Chemical Sciences Development and characterisation of oral fast dissolving tablet of nifedipine using camphor as a subliming material

ABSTRACT Mouth fast dissolving drug delivery system has gained high patient acceptability and popularity in the recent times. The aim of this study was to evaluate the effect of increasing nifedipine load on the characteristics of fast-disintegrating sublingual tablets for the potential emergency treatment of anginal pain and hypertension. Nifedipine undergoes first pass metabolism in liver and gut wall which has oral bioavailability of 43-77%. Sublingual dosage form bypasses the metabolism of the nifedipine in liver and offers a fast relieve from anginal pain and hypertension. An attempt has been made to prepare fast dissolving tablets of nifedipine were prepared by wet granulation technique using camphor as subliming agent and sodium starch glycolate together with crosscarmellose sodium as superdisintegrants, flavor and sweetner impart the taste to the formulation. The porous granules were compressed in to tablets by single punch tablet machine. Camphor was sublimed from the tablet by exposing to vacuum drier at 60°c for 12 hrs. All the formulations were evaluated for weight variation, hardness, friability, content uniformity, wetting time, disintegration time and dissolution rate. Among the formulations, (NEF6) one containing to be the best acceptable in terms of palatability, fast dissolving tablet having adequate strength. The disintegration time was found to be 58.0 ± 0.4 seconds, hardness of 3.4 ± 0.41 kg/cm2, wetting time of 39.3 ± 1.80 sec and drug release of 99.96% in 10 mins. All the formulations showed low weight variation. The present study demonstrated potentials for rapid absorption, improved bioavailability, effective therapy and patient compliance

COMPARATIVE IN-VITRO ANTIBACTERIAL AND ANTIFUNGAL ATTRIBUTES OF DIFFERENT SOLVENT EXTRACTS FROM LEAF, BARK, ROOT AND INFLORESCENCE OF MEMECYLON UMBELLATUM BURM.

This paper describes the antibacterial and antifungal activities and Minimum Inhibitory Concentration (MIC) of different solvent (pet. ether, chloroform, ethyl acetate, acetone, methanol and water) extracts of leaves, bark, root and inflorescence of Memecylon umbellatum burm. The percent yields from leaves, bark, root and inflorescence was found to be 0.2062 to 2.836, 0.0601 to 0.5142, 0.050 to 1.425, 0.0210 to 0.717 respectively. Overall, acetone extract produced from the leaves exhibited significantly (P &lt; 0.05) higher antibacterial activity along with superior antifungal activity. MIC for acetone and ethyl acetate extract of leaf was found to be 0.5 mg for the entire organisms compared to 3-15 mg for other extracts. Such study will explore pharmacological activity of the tested parts of Memecylon umbellatum burm especially, the leaves which might be valuable for therapeutic applications

Colorimetric method for simultaneous estimation of amlodipine besylate from plasma

Aim: The present work was to develop the method of analysis which can estimate drug in combined form without prior separation. Materials and method: By using UV spectroscopy colorimetric method was used for determination of Amlodipine besylate (AML) from plasma. Result and conclusion: This method is based on the formation of green colour in reaction between AML and 0.4 % Ferric chloride (FC) and 0.2 % Potassium ferricyanide (PF).The absorbance was measured at 775 nm. Result of tablet analysis showed % S.D. values in the range of 098.22 to 100,63%. Standard deviation value for tablet analysis by using methanol ranging from 98.01 to 101,13 % which proves the ability of the method to remain unaffected by small but deliberate change in reaction conditions and this method is used for estimation of AML from biological samples.Objetivo. El objetivo del presente estudio era desarrollar un método de análisis que permitiera estimar la cantidad de fármaco en forma combinada sin separación previa. Material y Método. Se utilizó espectroscopía colorimétrica UV para la determinación de Amlodipino Besilato (AML) plasmático Resultados. El presente método está basado en la formación de color verde en la reacción entre Amlodipino Besilato (AML) y cloruro férrico 0,4% y ferrocianuro potásico 0,2%. La medida de la absorbancia se realizó a 775nm. El resultado del análisis de los comprimidos mostró unos valores de DE comprendidos entre 098,22 y 100,63%. El valor de la DE utilizando metanol oscilan entre 98,01 y 101,13% lo que demuestra la capacidad del método de permanecer inalterado por pequeños pero intencionados cambios en las condiciones de la reacción, este método es usado para la estimación de Amlodipino Besilato (AML) en muestras biológicas

Phytochemical screening and In Vitro Antioxidant potential of Memecylon umbellatum Burm leaf extracts

Objective: Different dry extracts of Memecylon umbellatum Burm leaf obtained by various solvents such as petroleum ether, chloroform, ethyl acetate, acetone, methanol and chloroform water (IP) was screened to reap the benefits of its antioxidant and free radical scavenging properties using ascorbic acid as standard antioxidants. Methods: The in vitro free radical scavenging activity was evaluated using diphenyl picryl hydrazyl (DPPH) radical method using various concentrations of dry extract in distilled water (1, 2, 4, 8, 16, 20 μg/ml) against blank with ascorbic acid as a standard in same concentrations. Results: Among the all extracts, Methanol leaf extract has showed higher Antioxidant activity (84.65 ± 0.064 %) having IC50 Value 11.81 ± 0.033 μg/ml at 20 μg/ml. While, IC50 value for ascorbic acid was found to be 8.91 ± 0.084 μg/ml. Conclusion: The results clearly indicate that Methanol leaf extract of Memecylon umbellatum is effective in free radical scavenging. So in future, this may emerge as promising natural herbal source of powerful antioxidant. Keywords: Memecylon umbellatum, DPPH reagent, Antioxidant activity, Ascorbic acid, IC50

Evaluation of acute oral toxicity of the Camellia sinensis phytosome formulation in female wistar rats

Acute toxicity study was carried out for evaluation of toxic effect of formulation, safe acute dose for human and potential target organ for toxicity. Tea (Camellia sinensis), a cultivated evergreen plant and belonging to Theaceae family. The goal of present investigation was to perform acute toxicity study of Camellia sinensis phytosome formulation (CSP) for estimation of LD 50 or Median fatal dose and safe acute dose for human. A total of 12 female wistar rats weighing 90 to 100 gm were used in this investigation and divided into four groups, each with three animals, in accordance with 423 OECD guidelines. Group 1, 2, 3 and 4 animals were orally administered with 300 mg/kg bw of CSP, 300 mg/kg bw of CSP, 2000 mg/kg bw of CSP and 2000 mg/kg bw of CSP respectively. All the animals were observed for clinical sign, symptoms, body weight changes and mortality for 14 days. There was no death in any of the animals, and there were no significant variations in clinical signs or body weight in the experimental group. There were no abnormal alterations found during a gross necropsy.&nbsp

Microscopic Evaluation of Leaves of Memecylon umbellatum Burm

Objective. Aim of present work is to perform the microscopic evaluation and physicochemical analysis and to explore the morphology parameters of Memecylon umbellatum Burm leaves. Methods. Fresh, dried and desiccated powdered leaf samples were studied for their morphology, microscopy, organoleptic characters, and an assortment of other WHO recommended methods for standardisation. Results. The microscopy revealed the dorsiventral nature of the leaf. Midrib showed presence of nonlignified phloem, lignified xylem with well-defined xylem fibers, vessels, and parenchyma. Presence of Phloecentric vascular bundles surrounded by endodermis and crystal sheath. Well-defined patches of collenchyma were observed above and below the vascular bundles in the midrib area. Trichomes are mostly absent and stomata (anomocytic) were observed on both epidermal surfaces. Conclusions. It can be concluded that the microscopic analysis and pharmacognostic parameters can serve as tool for developing standards for proper authentication, quality, and purity of Memecylon umbellatum Burm leaves

Synthesis, Characterization and Evaluation of Analgesic and Anti-inflammatory Activities of Some Novel Indoles

Purpose: Long-term clinical usage of nonsteroidal anti-inflammatory drugs (NSAIDs) is associated with significant side effects - gastrointestinal lesions, bleeding and nephrotoxicity. Therefore, the discovery of new safer antiinflammatory drugs represents a challenging goal for this research area. Methods: Various derivatives of 3-(2-aminopyrimidin-4-yl) indoles viz. 4-(4-substitutedphenyl)-6-(2-(4 substitutedphenyl)-1H-indol-3-yl) pyrimidin-2-amine (4a-4r) were synthesized by cyclization of (3-(4- substitutedphenyl)-1-(2-(4-substitutedphenyl)-1H-indol-3-yl) prop-2-en-1-one) of indole with guanidine hydrochloride in the presence of sodium isopropoxide. Their structures were confirmed by FTIR, 1H NMR and elemental analysis. These compounds were investigated for their analgesic, inflammatory and ulcerogenic activities. Results: All the compounds tested (4a-4r) showed analgesic and inflammatory activities. Seven compounds (4d, e, h, j, k, q, p) out of 18 compounds showed antiinflammatory activity comparable to that of the reference standard, indomethacin, but with much lower ulcerogenic action. Compounds 4j and 4k showed 87.4 and 88.2 % inhibition of paw edema, 78.5 and 76.6 % protection against acetic acid-induced writhings and 0.89 and 1.12 of severity index, respectively, compared to 92.7 %, 82.8 % and 2.2, respectively, for indomethacin. Conclusion: The results show that incorporation of an appropriately substituted pyrimidine ring in indole nucleus can afford molecules with good analgesic and anti-inflammatory activities but with reduced gastric irritation