Volume 3

July-September 2011

Review Articles

Amit Jain

The purpose of writing this review on floating drug delivery systems (FDDS) was to compile the recent literature with special focus on the principal mechanism of floatation to achieve gastric retention. Several approaches are currently utilized in the prolongation of the GRT, including floating drug delivery systems (FDDS), also known as hydro dynamically balanced systems (HBS), swelling and expanding systems, polymeric bioadhesive systems, modified-shape systems, high-density systems, and other delayed gastric emptying devices. From the formulation and technological point of view, the floating drug delivery system is considerably easy and logical approach. An attempt has been made in this review article to introduce the readers to the current technological developments in floating drug delivery system.

Keywords: Floating Drug Delivery System, Single Unit, Multiple Unit, Gastric Retention Time.

J S Mulla , I M Khazi , Naveen Kumar Sharma , S P Hiremath , V G Jamakandi

Solid lipid nanoparticles (SLN) introduced in 1991 represent an alternative carrier system to traditional colloidal carriers, such as emulsions, liposomes and polymeric micro- and nanoparticles. The SLN combine the advantages (e.g. physical stability, protection of incorporated labile drugs from degradation, controlled release, excellent tolerability) of other traditional colloidal systems. This review describes the different ways of SLN production such as high pressure homogenization, ultrasonication, solvent emulsification/ evaporation, microemulsion, spray drying and double emulsion method.

Keywords: Solid Lipid Nanoparticles, High Pressure Homogenization, Ultrasonication, Solvent Emulsification/ Evaporation Micro Emulsion, Spray Drying, Double Emulsion.

Research Articles

Hui-Juan Liu , Ping Li , Yu-Min Li

A novel magnetic/pH sensitive chitosan/alginate (Chi/Alg) hydrogel bead was prepared by the L9 (34) orthogonal Test (four factors: The alginate concentration, chitosan concentration, CaCl2 concentration and weight ratio of Fe3O4 to polymer; three levels.) for controlled the delivery of carbamazepine (CBZ). Structure and surface morphology of the hydrogel were characterized by FTIR, SEM and magnetic property, respectively. In addition, the delivery behavior of carbamazepine from the hydrogel bead was studied. The CBZ cumulative release amount in pH 1.5 was smaller than in pH 6.8, the sequential release circumstance showed that the released amount of CBZ was 22.77% within 2 h and 91.63% after 24 h. The release of carbamazepine from the hydrogel bead at various pH values was analyzed by a semi-empirical equation, and it was found that the drug release mechanisms were either “anomalous transport” or “case-II transport”. The hydrogel bead possess magnetic property. The results clearly indicated that the hydrogel bead occupate magnetic/pH sensitivety, the magnetic/pH sensitive chitosan/alginate hydrogel bead may be a potential polymeric carrier for controlled the delivery of carbamazepine. This study may become an important experimental evidences of preparing an implantable magnetic nano-drug delivery system for treatment of the epilepsy.

Keywords: Carbamazepine, Hydrogel, Delivery Properties, Chitosan, Superparamagnetic.

Lian-Dong Hu , Wei Liu, Jian-Xue Yang, Li Li,

The purpose of this study was to prepare and evaluate the gastric floating microspheres of dextromethorphan hydrobromide that would prolong the gastric residence time and continuously release the drug in controlled manner. These microspheres were prepared by emulsion-solvent diffusion technique using ethyl cellulose (as carrier polymer) with drug in a mixture of dichloromethane and ethyl acetate. The physico-chemical properties of microspheres such as floating ability, drug loading, entrapment efficiency and in vitro drug release were investigated. The central composite design was chosen to obtain the optimum formulation. The microspheres prepared with optimal formulation were spherical with a size distribution range between 45 and 200 μm. The floating rate after 24h was (76.59±6.53) %, and the drug loading capacity and entrapment efficiency was found to be (13.79±0.93) % and (80.24±1.12) %.

Keywords: Floating Drug Delivery Systems, Floating Microspheres, Emulsion-Solvent Diffusion Method, Central Composite Design, Dextromethorphan Hydrobromide.

Awofisayo S O, Uwanta E J

The aim of the work was to detect and quantitatively assess the level of paracetamol in plasma samples of resident of the study area. Demographics of users and factors relating to the use are also examined. Plasma and urine samples were collected from 87 volunteers among buyers at a pharmaceutical care unit. The samples were screened for the presence of paracetamol and subsequently analyzed for the amount of paracetamol by colorimetric approach using Glynn and Kendal’s method. Urine screening for paracetamol indicated a positive test for 80.4% of the samples. Prescriptions in the hands of volunteers had 49.3% features of paracetamol. The correlation between respondents screened positive for paracetamol and handling paracetamol containing prescription was 0.72. The range of paracetamol levels observed in plasma was 110-490 µg/ml. Routine screening of patients prior to dispensing of paracetamol in pharmaceutical care centres is imperative for control of possible liver damage due to continuous use and resulting accumulation of paracetamol and its metabolite in blood.

Keywords: Colorimetric Approach, Paracetamol, Detection, Plasma Levels, Pharmaceutical Care.


Kesari Asha, Dash V, Maiti B C

One of the advanced research areas of herbals includes use of advanced formulation techniques for delivering herbal actives. Various herbal drugs become less utilized due to their poor absorption and poor bioavailability after oral administration. The problem can be resolved by opting a suitable delivery system which can enhance the rate and extent of drug solubilising into aqueous body fluids as well as its ability to go through lipophilic biomemebranes. Here we have formulated calcium alginate beads loaded with petroleum ether extract of Murraya koenigii by using Orifice Gelation Technique for improving their therapeutic indices and their efficacy. A series of batches was prepared to optimize the polymer: drug ratio and the beads were evaluated for physical characteristics like percentage yield, entrapment efficiency, moisture content, micromeretic properties, scanning electron microscopy (SEM), swelling ratio, compatibility studies, X-Ray Diffraction (X-RD) and in vitro drug release studies. The beads showed the mean particle size of 994-1290μm. SEM studies revealed that the beads were spherical with nearly smooth surface. FT-IR studies revealed that there was no polymer drug interaction. Application of in vitro drug release data to various kinetic equations indicated first order release.

Keywords: Murraya Koenigii, Calcium Alginate Beads, Orifice Gelatin Technique, In Vitro Drug Release.

C N Okwuosa, N C Azubike, Ii Nebo

The effect of the aqueous and methanol extracts of Sida acuta on blood glucose levels in both normal and diabetic rabbits was studied. The leaf extracts were screened for their effects on blood glucose levels in glucose overloaded rabbits. These extracts were also tested for anti-diabetic activity in alloxan-induced diabetic rabbits. Acute toxicity and preliminary phytochemical studies were performed. Results showed that both the aqueous extracts of S acuta (AESA) and the methanol extracts of S acuta (MESA) (400mg/kg) significantly increased the tolerance for glucose in glucose fed normal rabbits. Blood glucose was reduced significantly at 11/2 hrs post-glucose load (p<0.05). This reduction was consistent and persisted to 21/2 hrs. The positive control drug (glibenclamide, 0.5 mg/kg body weight, p.o) produced significant reduction on glycemia at 2 hours post glucose load (p<0.01). The methanol extract produced a significantly lower glucose concentration (mg.min/dl), as calculated from the area under the curve (AUC) of the glucose tolerance test, than AESA, glibenclamide and negative control respectively in the time periods 30-60 minutes, 60-90minutes and 90-150minutes (p<0.05; p<0.01). Both extracts (AESA and MESA) reduced blood glucose level in alloxanized rabbits significantly (p<0.05). The AESA and MESA (400mg/kg p.o) produced significant decreases in blood sugar at 4hours with percentage glycemic change of 30% and 20% respectively. The anti-hyperglycemic action of AESA and MESA were sustained up to 8 hours with significant percentage glycemic change of 46% and 45% respectively (P<0.01). Glibenclamide (0.5 mg/kg p.o) produced significant glucose reduction in alloxanized rabbits at 2 hours with a percentage glycemic change of 24.5% (P<0.01) and a percentage glycemic change of 40.4% at 8 hours. The crude leaf extracts of Sida acuta possess anti-hyperglycemic activity in diabetic and normal glucose fed rabbits.

Keywords: Sida acuta, Extracts, Alloxan, Anti-hyperglycemia.

Ganesh Krishnamoorthy, Sridharan M, Umamaheswari Krishnan, Swaminathan Sethuraman

Aerobic microorganisms are responsible for majority of infections. By means of formation of biofilms, resistance against various drug delivery systems are been reported. Most of the aerobic microorganisms are catalase and superoxide dismutase positive. The main objective of this study is to create antibiotic loaded implants, which releases antibiotics during the presence of aerobic microorganisms, thereby preventing the formation of biofilms and improving the treatment efficacy. Stainless steel plates were coated by dip coating method. The solution was prepared by using Polyhydroxybutyrate-co-hydroxyvalerate in Dichloromethane and followed by addition of ofloxacin. By spray coating technique, sodium formate was coated over the polymer film. Parameters such as in vitro drug release, zone of inhibition were studied. Coated plates with uniform thickness of 9µm were obtained. In all bacterial strains, Staphylococcus aureus, Clostridium sporogens, Pseudomonas aeruginosa, the zone of inhibition was noticed with a inhibited zone area of 64mm for S. aureus and 19mm for C. sporogenes. The in vitro drug release study showed that the total encapsulated drug was released over a period of 6 hours. Antibiotic coated plate’s offers a new perspective for treating implant related infections and also overcoming formation of biofilms. The study can be applied for creating biosensors to detect microorganisms.

Keywords: Aerobic Organisms, Catalase, Infections, Superoxide Dismutase, Ofloxacin.

Short Communications

Kamal Dua, Kavita Pabreja

Ursodeoxycholic acid (UDCA) is a water insoluble drug used for the dissolution of cholesterol gallstones because it reduces the cholesterol saturation of bile along with the treatment of other liver diseases, such as primary biliary cirrhosis, chronic hepatitis and biliary pains. However in vivo studies have shown that intestinal absorption and consequently the bioavailability of the drug are generally poor and erratic both among different subjects, and within the same subject. More than 50% is lost in the stool after a single oral dose of 300 mg. Aqueous solubility of UDCA was enhanced by preparing its solid dispersions using polyvinyl pyrrolidone (PVP) as water soluble carrier and cyclodextrin complexes with β-cyclodextrin. Absorption studies using in-situ rat gut technique exhibited greater rate of intestinal absorption with solid dispersions of UDCA when compared with βcyclodextrin. The intestinal absorption followed the first order rate kinetics. Statistical correlation of in vitro drug dissolution and in vitro drug absorption indicates a positive correlation. This increased absorption may be due to the solubilisation and improved wetting of UDCA in PVP rich micro-environment.

Keywords: Ursodeoxycholic Acid, Solid Dispersion, Complex, In-situ.

Ajeet , Rohit Chaudhary, Arvind Gupta, Santosh Kumar Ram

The purpose of present work was to design and evaluate mucoadhesive placebo buccal devices. These patches are composed of mixture of mucoadhesive polymer Methyle cellulose and water in combination with Polyvinylpyrollidone and glycerin. The patches were fabricated by solvent casting techniqu and were evaluated for its physical properties. The patches were evaluated for film weight uniformity, thickness, swelling index, surface pH, mucoadhesive time and folding endurance. A combination of Methyle cellulose with Polyvinylpyrollidone K30, glycerin with water as solvent gives promising results.

Keywords: Mucoadhesive, Placebo, Solvent Casting Technique, Methyle Cellulose, Water.

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