Determination of Hydrophile - Lipophile Balance Value of Raphia hookeri Mann (Family: Palmae) Gum by Emulsification Method

Background: The hydrophile-lipophile balance (HLB) value is the major determinant of the applications of surfactants and any material that has potential for surface activity.Objective: To determine the HLB value of Raphia hookeri Mann (Family: Palmae) gum by emulsification method.Methods: Exudates of Raphia hookeri were collected and the gum was extracted and purified via dissolution in water, precipitation using ethanol, defatting using diethyl ether, oven-drying and pulverization. The pH and viscosity of 3 %w/v dispersion of the gum were determined in comparison with those of Tween 80 and Span 60. Series of emulsions were formed with the gum and Tween 80 as well as the gum and Span 60, in varying ratios of 1:5, 1:2, 1:1, 2:1 and 5:1. The emulsions were kept for 5 days at room temperature after which they were assessed for stability by checking the extent of creaming. The most stable emulsion was selected and the fractions of gum and standard surfactant incorporated were used for calculating the HLB value of the gum.Results: The pH of 3 %w/v dispersions was in the order: Raphia hookeri gum < Span 60 < Tween 80 while the viscosity of the dispersion of Raphia hookeri gum was found to be more than four folds higher than those of Span 60 and Tween 80. The most stable emulsion was found to be the one containing Raphia gum and Tween 80 in ratio of 5:1 and the HLB value of the gum was found to be 11.44.Conclusion: Raphia hookeri gum is more acidic and produces more viscous dispersion compared to Tween 80 and Span 60. The HLB value of the gum falls within the range of 8 - 16 which is characteristic of oil-in-water emulsifiers.Keywords: Raphia hookeri Mann, Gum, Hydrophile-lipophile balance, Emulsification

Emulsifying Properties of Hemicelluloses

This chapter focuses on the emulsifying properties of hemicelluloses. Hemicelluloses are gummy polysaccharides of complexity between gum and cellulose. Based on the major monosaccharide constituents of their backbone, hemicelluloses can be classified into xylans, mannans, xylogalactans and xyloglucans. Their sources include seeds, husks, straws, leaves and wood. Hemicelluloses bring about emulsification by viscosity modification and by formation of multilayered films around each globule of the dispersed phase. They have strong emulsifying power but are somehow limited by batch-to-batch variation and susceptibility to microbial and chemical degradations. These limitations are overcome by the use of purified and semisynthetic derivatives. Hemicelluloses and derivatives herein considered for their emulsifying properties include those from barley straw, wheat straw, corn fiber, locust bean, guar, soy bean, konjac, prosopis seed and afzelia seed. Hemicelluloses, as plant polysaccharides, are only second to cellulose in terms of abundance. They have superior emulsifying properties compared to the typical gums. They are amenable to many chemical modifications for the enhancement of stability and for the improvement of emulsifying properties. Hemicelluloses were not given adequate attention in the past; but this chapter shows that they are potentially useful emulsifying agents

Lubricating Effects of Cocoa Butter and Coconut Oil in Conventional Paracetamol Tablets

Background: Due to chemical instability of some Active Pharmaceutical Ingredients often caused by magnesium stearate and its impurities, it is expedient to research into some other materials especially of natural origin, which would probably exhibit better lubricating activity, chemically inactive, less bioactive and less prohibitive.Objective: This work is designed to examine the lubricating properties of cocoa butter and coconut oil as alternative lubricants in comparison with conventional lubricant - magnesium stearate at different concentrations in paracetamol tablets.Materials and Methods: Cocoa butter was extracted from the seeds of Theobroma cacao and coconut oil from the meat of matured coconuts harvested from the coconuts palm (Cocos nucifera). Physicochemical evaluation was carried out on the extracted oils. Thirteen different formulations were prepared using different lubricants; magnesium stearate, cocoa butter and coconut oil at 0 – 4 %w/w concentrations. The prepared granules were evaluated for various pre-compression characteristics (bulk density, tapped density, angle of repose, Hausner’s quotient and Carr’s index) and post-compression characteristics (weight variation, friability, hardness, disintegration and dissolution times).Discussion: Most of the values obtained from the evaluation of pre- and post- compression characteristics correlate with the pharmacopoeial limits. The values of disintegration time were observed to increase as the lubricant concentration increased but no direct relationship with dissolution time. Tablet hardness values decreased while friability increased as the lubricant concentration increased for all the batches. From the study, cocoa butter and coconut oil at 2 – 4 % exhibited effective lubricating effect in the formulation of paracetamol tablet with respect to their values of weight variation, friability, hardness, disintegration and dissolution times.Conclusion: Cocoa butter and coconut oil could be employed as good alternative lubricants to the conventional ones in pharmaceutical tablet formulation.Keywords: Lubricants, Cocoa butter, Coconut oil, Magnesium stearate

Dissolution and permeation characteristics of artemether tablets formulated with two gums of different surface activity

Purpose: To evaluate the dissolution and permeation characteristics of artemether tablets formulated with cashew and prosopis gums, and compare with tablets prepared with acacia gum.Methods: Artemether tablets containing varying concentrations (1.0 to 4.0 %w/w) of cashew and prosopis gums or 3 %w/w of acacia (control) gum as binders were formulated by wet granulation method. The tablets were evaluated for crushing strength, friability and disintegration time. Dissolution and permeation characteristics of the formulations were studied using USP methods.Results: Tablets formulated with prosopis gum had higher crushing strength, higher friability and higher disintegration time compared to those of cashew gum at corresponding binder concentrations. Tablets formulated with 3 %w/w cashew gum exhibited complete drug release within 1 h, 95 % drug permeation in 188 min (in simulated gastric fluid [SGF]) and 95 % permeation in 224 min (under simulated intestinal fluid [SIF] condition) while those made with 3 %w/w prosopis gum exhibited 70.7 % drug release in 1 h, 95 % permeation in 135 min (in SGF) and 95 % permeation in 170 min (under SIF condition).Conclusion: Cashew gum is effective as a binder over a relatively wide range of concentrations to achieve fast drug release though with minimal permeation enhancement while prosopis gum is characterized by delayed drug release but enhanced permeation of the released drug.Keywords: Cashew gum, Acacia, Prosopis, Artemether, Drug release, Dissolution, Permeatio

Frequency and antibiotic susceptibility pattern of uropathogenic agents of urinary tract infections among asymptomatic diabetic patients in Okada community, southern Nigeria

Massive evidence showed that patients with diabetes have a high risk of urinary tract infections. We studied the frequency of potential urinary uropathogens among diabetic patients and identified their antimicrobial susceptibility patterns. This was a prospective hospital-based study conducted at the Department of Medical Laboratory Science, Igbinedion University Teaching Hospital, Southern Nigeria, between January 2014 and May, 2014. We included 240 previously confirmed diabetic patients (women, n=70 and men, n=170) who were regularly followed up without prior treatment with any antimicrobial therapy and within the age range of 26-75 years. Patient personal history data and midstream urine samples were collected. Urine samples were processed in the laboratory following a Standard Laboratory Protocol. Escherichia coli, Staphylococcus aureus, Klebsiella spp. and Candida spp. were isolated in this study. A significant bacteriuria count was estimated in 12.5% of the sampled population, while 17.1 and 10.6% were estimated in females and males, respectively. Similarly, candiduria was found in female, male and total sample in 12.9%, 2.9%, and 5.8%, in that order. According to antimicrobial sensitivity testing, the Gram-negative bacilli isolated were highly sensitive to nitrofurantoin followed by ofloxacin, gentamycin and least sensitive to cefuroxime. Estimation of potential uropathogens among asymptomatic diabetic populations may avert possible urinary tract infections and their possible complications ultimately and thus prevent possible advanced renal diseases

Expression Patterns of ER, PR, Her-2/neu and p53 in Association with Nottingham Tumor Grade: A retrospective hospital-based study

Objectives: Histological grading has been an integral part of cancer diagnosis for a long time. Recent molecular studies show that breast cancer is a heterogeneous disease, and several molecular changes may accumulate over time to influence treatment response. As a result, employing reliable molecular biomarkers to monitor these modifications may help deliver personalized treatment. However, this may be unrealistic in the resource-limited parts of the world. Thus, we studied the expression pattern of hormone receptors and p53 tumor suppressor using immunohistochemistry (IHC) in breast cancer (BC) compared to the traditional tumor grade. Methods: Two hundred and five (n =205) cases were investigated. The Modified Bloom-Richardson score system was adopted in grading the tumors. Tissue sections of the cases were stained with specific primary antibodies (at dilutions of 1:60 for estrogen (ER) and progesterone receptors (PR), 1:350 for human epidermal growth factor (Her-2/neu), and 1:50 for p53. The Chi-square test was used to determine the association between the tumor grade and IHC markers. Results: Invasive ductal carcinoma of no-specific type (190 cases;92.7%) was predominant. Grade II tumor (n =146; 71.22%) was the most frequent. Hormone receptors (ER+; n =227 and PR+; n =145) had 62.0% and 70.7% positive cases; 34.2% (n =70) were positive for Her-2/neu, while 76.1% (n =156) were positive for p53. We observed strong associations between Nottingham grade and expression patterns of ER (P ˂ 0.01), PR (P ˂ 0.001), Her-2/neu (P ˂ 0.001), and p53 (P =0.001). Conclusion: Nottingham grade has a high degree of concordance with the patterns of expression of hormone receptors, Her-2/neu, and p53, suggesting that it may play an important role in connection with the predictive and prognostic biomarkers for BC. Keywords: Breast cancer, Her-2/neu, hormone receptor, Nottingham grade, p53 mutation

Mucin-Grafted Polyethylene Glycol Microparticles Enable Oral Insulin Delivery for Improving Diabetic Treatment

In this study, different ratios of mucin-grafted polyethylene-glycol-based microparticles were prepared and evaluated both in vitro and in vivo as carriers for the oral delivery of insulin. Characterization measurements showed that the insulin-loaded microparticles display irregular porosity and shape. The encapsulation efficiency and loading capacity of insulin were >82% and 18%, respectively. The release of insulin varied between 68% and 92% depending on the microparticle formulation. In particular, orally administered insulin-loaded microparticles resulted in a significant fall of blood glucose levels, as compared to insulin solution. Subcutaneous administration showed a faster, albeit not sustained, glucose fall within a short time as compared to the polymeric microparticle-based formulations. These results indicate the possible oral delivery of insulin using this combination of polymers.Tertiary Education Trust Fund (TETFUND)–National Research Fund (NFR)Ministerio de Ciencia, Innovación y Universidade

EVALUATION OF CALLINECTES CHITOSAN AS A SUPERDISINTEGRANT IN METRONIDAZOLE TABLET

Objective: The objective of this study is to evaluate callinectes chitosan as a superdisintegrant in tablet formulation; superdisintegrants are incorporated into tablets at concentrations below 5% of tablet weight to effect prompt break-up of tablets after administration.Methods: Chitosan was extracted from shells of Callinectes gladiator. The polymer was characterized and then used as a disintegrant (in comparison with Ac-Di-Sol® and corn starch) at concentrations of 2, 4 and 8% for the formulation of metronidazole tablets. The micromeritic properties of granules; and mechanical and release properties of the tablets were studied.Results: A yield of 36.7% chitosan having degree of deacetylation of 62.7% was obtained from the crab shell. Fourier Transform Infrared absorption bands at 1495 and 3240 cm-1 typical of N-H bending and stretching respectively; and endothermic peak of 159 °C typical of melting of chitosan were obtained. No adverse interaction between the chitosan and metronidazole was observed. The disintegration times of tablets containing 2, 4 and 8% chitosan were 12.2, 10.4 and 9.3 min respectively.Conclusion: Callinectes chitosan is suitable for use as a superdisintegrant in tablets. It appears to be superior to corn starch as disintegrant although less effective compared to Ac-Di-Sol®. However, the relative cheapness and ready availability of chitosan would make it to be preferred to Ac-Di-Sol®

Research Article - Evaluation of the suspending properties of Albizia zygia gum on sulphadimidine suspension

Purpose: Some excipients are currently available for the formulation of pharmaceutical suspensions. The purpose of this study is to search for a cheap and effective natural excipient that can be used as an effective alternative for the formulation of pharmaceutical suspensions. Method: The suspending properties of Albizia zygia gum (family Mimosoideae) were evaluated comparatively with those of Compound Tragacanth, Acacia and Gelatin at concentration range of 0.5 - 4.0%w/v in Sulphadimidine suspension. Characterization tests were carried out on purified Albizia zygia gum. Sedimentation volume (%), rheology and particle size analysis were employed as evaluation parameters. The values obtained therefrom were used as basis for comparison of the suspending agents studied. Results: Albizia zygia gum is devoid of alkaloids, anthraquinones and carbohydrates which ensures its "inertness". Albizia zygia gum (2.5%w/v) produced a comparable suspending ability as 4%w/v Compound Tragacanth. Also, the suspending ability of all the materials was found to be in the order: Albizia zygia > Compound Tragacanth gum > Acacia gum > Gelatin. At all concentrations employed, Albizia zygia gum had the strongest suspending ability relative to the other materials. Conclusion: The results suggest that, due to the high viscosity of Albizia zygia gum, its mucilage can be a stabilizer of choice when high viscosity is desired. It can also serve as a good thickening agent in both pharmaceutical and food industries

Orally Administered Prosochit^®-Based Nanoparticles of Insulin Ameliorates Alloxan-Induced Diabetes in Rats

This work was aimed to assess the antidiabetic effect of orally administered Prosochit®-based nanoparticles of insulin in an animal model. Five batches of insulin-loaded nanoparticles were prepared as dry water-in-oil-in-water emulsions using different emulsifiers (prosopis gum, Prosochit® 201, Prosochit® 101, Prosochit® 102, and chitosan) for the outer emulsion. Unloaded Prosochit® 101-based nanoparticles were also formulated. The morphology and size distribution of the nanoparticles were studied using a scanning electron microscope and Zetasizer. Forty alloxan-induced diabetic Wistar rats were divided into eight groups. The different groups were administered daily with different formulations (unloaded nanoparticles, the 5 loaded nanoparticles equivalent to 50 IU insulin per kg, purified water, and Actrapid) for 14 days. Blood glucose level was monitored and determined over 24 h. Fasting blood sugar was also taken on days 3, 5, 7, and 14. A graph of the percent blood glucose level relative to time 0 h was plotted against time. The particles showed a water-in-oil-in-water constitution. Both the drug-loaded and the unloaded Prosochit®-based nanoparticles were of nano dimension. There was a significant difference (p ® 201, Prosochit® 102, and chitosan while the insulin-loaded Prosochit® 101 nanoparticles showed the best activity, which is comparable to subcutaneous insulin, reducing blood glucose levels to 32.20 ± 3.79%. All the oral Prosochit®-based insulin nanoparticles are characterized by appreciable antidiabetic activity with the activity of Prosochit® 101-based nanoformulation being comparable to that of the subcutaneous insulin