Volume 3

January-March 2011

Review Articles

Mahesh Dangi, Jyotsana Madan, Sagar Banode

Oral route continues to be the preferred route for most drug therapy. However, more than 40% of new chemical entities exhibit poor aqueous solubility, resulting in unsatisfactory oral drug delivery. Recently, much attention has been focused on Self emulsifying drug delivery systems and Self-Micro Emulsifying Drug Delivery System to improve the oral bioavailability of poorly aqueous soluble drugs. Self-micro emulsifying formulations and Self emulsifying formulations are mixtures of oils and surfactants, ideally isotropic, and sometimes containing co-solvents, which emulsify spontaneously to produce fine oil-in-water emulsion when introduced into aqueous phase under conditions of gentle agitation. The agitation required for self-emulsification is provided by the digestive motility of the stomach and intestine in vivo. When dissolution rate-limited absorption is seen, as in case of lipophilic drugs, Self emulsifying drug delivery systems and Self-Micro Emulsifying Drug Delivery System may be a promising strategy to improve the rate and extent of oral absorption. This review describes Self emulsifying drug delivery systems and Self-Micro Emulsifying Drug Delivery Systems used to formulate potent lipophilic drugs.

Keywords: Self-emulsifying, Self-micro Emulsifying, Lipid-based Systems, Poorly Soluble Drugs, Bioavailability.

Research Articles

Prajapati R K, Mahajan H S, Surana S J

In this study, a novel mucoadhesive microsphere for nasal administration was developed and investigated. The carvedilol loaded PLGA microspheres were prepared by a spray-drying technique that can be proposed as an alternative to the conventional methods for preparation of microspheres. The microspheres were evaluated with respect to the production yield, particle size, incorporation efficiency, swelling property, in vitro mucoadhesion, in vitro drug diffusion, ex-vivo permeation study, histopathological examination and stability study. Microspheres were characterized by differential scanning calorimetry, scanning electron microscopy and X-ray diffraction study to gain insights into the nature of interaction between the drug and polymer. It was found that the particle size, swelling ability and incorporation efficiency of microspheres increases with increasing drug to polymer ratio. Microspheres show adequate mucoadhesion and do not have any destructive effect on nasal mucosa. The results of morphological examination indicated that the PLGA 50:50 microspheres possessed a smooth and spherical appearance with average particle size of 10-25 µm. Release profiles of carvedilol from the microspheres displayed an anomalous transport mechanism. The investigations of these microspheres as vehicle for nasal delivery showed that PLGA microspheres may be considered as a promising nasal delivery system.

Keywords: Carvidilol, Nasal, PLGA, Microspheres, Spray Drying.

Anand Gadad, Chirag Naval, Krunal Patel, Panchaxari Dandagi, Vinayak Mastiholimath

The present study was an attempt to develop floating microspheres of captopril to prolong its gastric residence time in stomach. Floating microspheres was formulated using biocompatible polymers like Eudragit S100 and Ethyl cellulose in different proportions by solvent evaporation technique. The prepared microspheres were evaluated for percentage yield, micromeritic properties, particle size, morphology, drug entrapment, buoyancy studies, In vitro drug release studies. Practical yield of the microspheres was up to 76.40%. The formulated microspheres were free flowing with good packing properties. Scanning electron microscopy confirmed spherical structure and the particles were of the size range of 57.66 to 93.21µm. The microspheres with Ethyl cellulose showed higher buoyancy when compared with Eudragit S-100. All formulation showed good in vitro percent buoyancy. In vitro release studies showed cumulative % drug release between 75.95-88.27%. In vitro release studies demonstrated non-Fickian diffusion of drug from the microsphere.

Keywords: Floating Microspheres, Captopril, Eudragit S-100, Ethyl Cellulose.

Sunday Olajide Awofisayo, Nse Okon Eyen, Aniefiok Jimmy Uwah

This study examines the pattern of prescribing, adequacy of community based pharmaceutical care and patient’s presenting diastolic blood pressure as a pointer to possible therapeutic success in Akwa Ibom state, Nigeria. Six community pharmacy outfits were visited to meet buyers who are hypertensive having duly signed prescriptions. Questionnaires were administered seeking information on the demographics and behavioural diposition of respondents to their drugs and assessment of care concern of the pharmacist in charge of their prescription fill. Seven hundred and sixty seven respondents, males (32.0±7.6) and females (39.0±6.8) predominantly natives of Akwa Ibom participated in the study. 11.1% of the respondents were underweight while 29. 5 were obese. The mean diastolic blood pressure (MDP) of obese males were significantly higher than their counterpart female BMI group (P>0.01). Only 24% of the respondent admitted knowledge of the professional services of a pharmacist and recorded a pharmaceutical care assessment of 24.98 ± 9.99 out of 50 points. The frequency of use of antihypertensive was diuretic, anxiolytic, beta-receptor antagonist, ACEI and other classes in the order 36.0%, 27.9%, 15.4%, 13.9% and 5.8% respectively. The monitoring of drug use pattern as part of pharmaceutical care in hypertensive patients can make readily available information on which improved patient care is based in that environment.

Keywords: Hypertension, Pharmaceutical Care, Prescriptions.

Preeti Garg, Divay Gandhi, Pankaj Khatri, Anupriya Pandey, Vaibhavi Jakhetia

Capparis decidua (Forsk) Edgew. Belongs to family Capparaceae, a small much branched tree. The plant possesses anthelmintic, hepatoprotective, antidiabetic, hypolipidemic activity. Pharmacognostic investigation of fresh, powdered and anatomical sections of stem were carried out to determine its macromorphological, micromorphological and chemomicromorphological profiles. Phytochemical investigation indicated the preparation of different extracts using different solvents and different tests were carried out for confirmation of alkaloids, tannins, phenolic compound, flavanoids, steroids, glycosides & carbohydrates. The result of the study can be useful in setting some diagnostic indices for the identification and the preparation of the monograph of the plant.

Keywords: Capparis decidua, Capparaceae, Pharmacognostic, Phytochemical Investigation.

D C Nwachukwu, C N Okwuosa, P U Chukwu, Nkiru Azubuike Nkiru, T Udeani

The hepatoprotective activity of methanol extract of seeds of Sesamum indicum was investigated in carbon tetrachloride (CCl4) induced liver injury in rats. The rats were divided into six (6) groups (A-F) of five each. Graded doses (200, 400, and 800 mg/kg) of methanol extracts of seeds of Sesamum indicum (MESI) were administered orally to three different groups (A-C) respectively for seven days prior to CCl4 injection. Groups D and E received 5mL/kg of physiological saline and 50 iu/kg α-tocopherol respectively using oral gavage while the last group (F) served as the baseline control group. On the 8th day, animals in all the groups except group F were given carbon tetrachloride (2 mL/kg body weight) in olive oil subcutaneously. Twenty four (24) hours later, blood was collected from all the groups by retro-orbital puncture for liver marker enzyme determination. Liver was excised for histopathology. Results showed significant increase in the levels of biochemical markers of hepatic damage like alanine transaminase (ALT), aspartate transaminase (AST), and alkaline phosphatase (ALP) in CCl4 control group (D) when compared with the baseline control group F (p < 0.001). Treatment with MESI (200, 400, and 800 mg/kg) prior to CCl4 administration, significantly protected rats from injury as evident by moderate changes in liver histoarchitecture in groups A-C and significant reduction(p˂ 0.001) in levels of ALT, AST and ALP when compared to the CCl4 control group. The CCl4 control group showed marked vacuolar degeneration, inflammatory cell infiltration, and necrosis of hepatic tissue. The methanol seed extract of Sesamum indicum possess hepatoprotective activity.

Keywords: Sesamum indicum, Methanol Extract, Hepatotoxicity, Biochemical Markers, CCl4.

Panchaxari Dandagi, Punit Patel, Pravin Patil, Vinayak Mastiholimath, Anand Gadad

In the present study polymeric biodegradable nanoparticles (NPs) of Etoposide (ETP) were prepared by modified spontaneous emulsification solvent diffusion method using polylactic-co-glycolic acid (PLGA) as biodegradable matrix. The formulations were then characterized with respect to size and its surface morphology, zeta potential, entrapment efficiency, in vitro drug release profile, sterility testing, stability studies and in vivo tissue distribution study. The formulated Etoposide-PLGA nanoparticles were spherical with a diameter ranging from 150 to 250 nm. Highest entrapment efficiency was found to be 73.83%. Highest cumulative percent drug release was observed with F-8 (83.50%) in 120 hrs. Formulation F-8 with optimal particle size, high entrapment efficiency and satisfactory in vitro release was selected for in vivo studies. The average targeting efficiency of drug loaded nanoparticles was found to be 27.23±0.126% of the injected dose in liver, 41.72±0.415% in lungs, 10.63±0.269% in kidney and 13.24±0.572% in spleen. The results revealed that, the drug loaded nanoparticles showed preferential drug targeting to lungs followed by liver, kidney and spleen. Stability studies indicated that 4°C is the most suitable temperature for storage of PLGA nanoparticles. This drug delivery is endowed with several exclusive advantages and hence holds potential for further research and clinical application.

Keywords: Etoposide, PLGA, Biodegradable Nanoparticles, In Vitro Release, In Vivo Study.

Debajyoti Ray

Nanocomposite of 2-Ethyl hexylacrylate (EHA) and acrylic acid (AA) intercalated with sodium silicate (SS) was prepared by emulsion technique using benzoyl peroxide (BPO) as reaction initiator. The transmittance electron microscopy showed the well dispersion of the polymer nanocomposite into the intercalated silicate layers. The novel nanocomposite was further characterized by NMR, IR, TGA and exhibited excellent properties of higher thermal stability and super absorbency for use as high performance materials. P(EHA-co-AA)/silicate nanocomposite was found to have better swelling capacity in simulated intestinal fluid. So the nanosystem is expected to be useful as controlled drug delivery device in future.

Keywords: Intercalation, Nanocomposite, Swelling Studies, Degradation Studies.

Short Communications

Kamal Dua, Kavita Pabreja, Vinny Lather

Aceclofenac (AF) is a new generational non-steroidal anti-inflammatory drug showing effective anti-inflammatory and analgesic properties with a good tolerability profile in a variety of painful conditions like ankylosing spondylitis, rheumatoid arthritis and osteoarthritis. Aceclofenac is very slightly soluble in water and therefore an attempt has been made to prepare inclusion complexes of aceclofenac with β-cyclodextrin (β-CD) and to explore the possibility of its molecular arrangement using molecular modeling and structural designing. The results indicated the relative energetic stability of the β-CD dimer-AF complex as compared to β-CD monomer-AF. Such molecular-modeling studies can be employed as an additional tool to support the formation of stable molecular inclusion complexation of any water insoluble drug complexed with cyclodextrins.

Keywords: Aceclofenac, β-cyclodextrin, Molecular, Modeling.

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