Volume 12, Issue 1, Jan-Mar 2020

Volume 12

January-March 2020

Resealed erythrocytes as drug carrier

Bhawana Sharma, Amul Mishra, Piush Sharma, Savita Rathore, Shiv Kumar Garg, Abhishek Dwivedi

Abstract:
Resealed erythrocytes hold vital position owing to their many advantages like biocompatibility, biodegradability, long circulating half-life and versatility of carrying different drugs with better entrapment efficiencies. By exploitation of various chemical and physical methods (hypotonic dilution, hypotonic hemolysis, electro-insertion, endocytosis, hypoosmotic lysis) the cells are broken and the drug is entrapped into the erythrocytes, finally they are resealed and the resultant carriers are then called “resealed erythrocytes”. These drug carriers are rapidly taken up from blood by macrophages of reticuloendothelial system present in liver, lung and spleen and are prepared by collecting blood sample from the organism &separating erythrocytes from plasma. Wide varieties of drugs like Antiinflammatory, steroidal and chemotherapeutic agents are seen to have reduced side effects upon incorporation into these carriers. The main objective of this review is to explore the source and isolation, drug loading technology, characterization, biomedical application and future aspects of resealed erythrocytes.

Keywords: Resealed Erythrocytes, Biocompatible, Carrier, Applications, RES.

Development and evaluation of fast disintegrating tablets of valsartan ‎for orodispersible using ‎superdsintegrants, mannitol and polyethylene ‎glycol 4000‎

Abiodun O Shittu, Ngaitad S Njinga, Abdulghazal Olawale

Abstract:
Over the past two decades, fast disintegrating tablets have gained global attention as a fast-rising alternative to conventional tablets by providing solutions to the limitations and disadvantages of earlier dosage forms administered orally. Valsartan sodium was formulated into tablets using the direct compression method. Different formulation batches were developed. Batches A1 to A3 contained fixed API, sodium starch glycolate, cellactose and mannitol in varying proportion; B1 to B3 contained fixed API, croscarmellose sodium, cellactose, and PEG 4000; C1 to C3, contained fixed API, SSG, cellactose, mannitol and PEG 4000 (50:50); D1 to D3 contained fixed API, CCS, cellactose, MN and PEG 4000 (50:50). The pre formulation characteristics of all powder mixtures showed good flow and compressibility properties. Batches A1 – A3 tablets containing mannitol were harder than B1 – B3 containing PEG 4000. From the results, C1 and D1 contained both MN and PEG 4000 in different proportion, PEG was responsible for lower tablet hardness, while both excipients played positive role in lowering disintegration time, C1 with average hardness and lower DT (47 .53 N, 6.44 s) will be adequate for FDT design for mouth disintegration on one hand, and A2 or A3 with hardness and DT:107.8 N, 7.21 s and 91.54 N, 6.80 s respectively could be best applied for the FDT intended to withstand rough handling transportation for commerce. The FTIR analysis of batches A to D showed no changes in the API peaks when compared with that of valsartan drug.

Keywords: Valsartan, Mouth Disintegrating, Fast Disintegrating, Rapid Disintegrating, Orodispersible.

Formulation development and in vitro characterization of oral floating ‎in situ gelling ‎liquid system of rivastigmine tartrate

Aarthi C K, Elango K, Daisy Chellakumari S, Nithya S

Abstract:
The main aim of the study was to develop a stable gastroretentive In situ gel of Rivastigmine tartrate for Geriatric patients in the treatment of Alzheimer’s disease. Rivastigmine tartrate oral In situ gel was formulated by pH-triggered ionic gelation using various gelling polymers such as Sodium alginate, Gellan gum and Iota carrageenan along with HPMC K4M as release retardant. Prepared formulations were evaluated for Physical appearance, Pourability, pH, viscosity, In vitro gelation study, In vitro buoyancy study, Density, Gel strength, Percentage water uptake, Drug content and In vitro drug release. All the parameters showed differences based on the combination and concentration of polymers used. The pH and drug content of the formulations ranged from 6.94 – 7.39 and 98.04 – 99.83 % respectively. All the formulations showed floating lag time of less than 2 minutes and the duration of floating was greater than 12 hours. In vitro drug release study showed that only the Formulations F9 and F10 released 99.91 % and 91.11% of drug respectively at the end of 12 hours, while the other formulations showed more than 90% of drug release even before the period of 12 hours. In vitro release kinetic study of the optimized formulation F9 showed that the formulation followed Zero-order kinetics and Non-Fickian diffusion mechanism. The stability studies indicated that the optimized formulation F9 remained stable at the end of 3 months. The formulated gastroretentive In situ gel prolonged the gastric residence time resulting in controlled delivery of the drug.

Keywords: In Situ Gel, Floating, Gastroretentive, Oral, Liquid, Rivastigmine Tartrate, Gelling Polymers, Alzheimer’s Disease.

Synthesis, antimicrobial activity and molecular docking study of monocarbonyl curcumin analogue ‎D125, D144, D156‎

Arief Kusuma Wardani, Ritmaleni, Erna Prawita Setyowati, Sardjiman

Abstract:
A novel curcumin analogue D125, D144 and D156 were developed to be potent antimicrobial against Gram positif and negative. Our work coupled both the tetrahydro-4H-thiopyran-4-one and new benzaldehyde derivatives by using Aldol condensation protocol under acidic condition. Three series of the curcumin analogue were synthesized and characterized by IR, ¹HNMR, ¹³CNMR and Mass spectrometer analysis then evaluated for in vitro antimicrobial activities. All the compounds were subjected to molecular docking studies for the inhibition of the cell wall bacteria, inside the active site of peptidyl transferase center of E. coli ribosome (PDB ID: 2EX8). Antimicrobial activities were tested using the serial difusion method. It was observed the most exhibited activity against the cell wall division is D156 with docking score (S) -11.7859. The test compound D144 exhibited moderate activities compared to the derivates compound whereas showed weak activities than HGV-6, D154 not exhibited activities compared to the derivates compound and HGV-6, D156 were more active than to the derivates compound and HGV-6. The trisubstituted D156 showed strongest antibacterial effects than the parent compounds HGV-6 and their derivates in Gram positive and negative but no activities against tested fungal strains.

Keywords: Synthesis, Antimicrobial Activity, Molecular Docking, Monocarbonyl Curcumin.

Formulation and evaluation of floating drug delivery system for cefuroxime axetil

Ashish Kumar Varma, Swatantra Kushwaha

Abstract:
The main aim of present study was to build up multiparticulate gastro retentive drug delivery system of Cefuroxime which is used to treat a wide variety of bacterial infections. This medication is known as a cephalosporin antibiotic. It works by stopping the growth of bacteria. The gastro retentive drug delivery system can be formulated to enhance the bio-availability of Cefuroxime Axetil by retaining the system into the stomach for extended period of time. Cefuroxime Axetil is a poorly water-soluble drug (BCS Class-II drug) and its bioavailability is exceedingly low. The rate of absorption and the extent of bioavailability for such insoluble drug are restricted by the rate of dissolution in the gastrointestinal fluids. The gastroretentive drug delivery system of Cefuroxime Axetil was primed by emulsion solvent diffusion method by using ethyl cellulose, Eudragit L100, HPMC, Chitosan polymers in changeable concentration. All formulations were evaluated for percent yield, particle size, entrapment efficiency, in vitro buoyancy as well as in vitro release studies. The resultant formulations showed superior buoyancy and in vitro controlled release of Cefuroxime Axetil.

Keywords: Floating Microsphere, Ethyl Cellulose, Hydroxypropylmethylcellulose (HPMC), Eudragit L100, Chitosan.

Design, development and characterization of fast dissolving oral film of clonazepam

Govind G Nikam, Jameel Ahmed S Mulla

Abstract:
The present study proposed to prepare fast dissolving oral film containing clonazepam for the treatment of epilepsy. HPMC E15 and PEG 400 were used as film forming agent and plasticizer, respectively. Solvent casting method was used to prepare Clonazepam loaded fast dissolving oral films. The prepared films were characterized for weight variation, thickness, percent elongation, tensile strength, folding endurance, moisture content, content uniformity, surface pH and swelling index. The DSC and FTIR Spectra revealed that drug was compatible with the polymer. The prepared oral films were opaque in nature having good folding endurance. Shows the rapid release of drug in oral cavity. Drug release by diffusion (93.44 %) and by dissolution (98.32%) after 5 minute. All nine batches are rapid release of drug after film contact with saliva.

Keywords: Clonazepam, Epilepsy, Fast Dissolving Oral Film, Solvent Casting, HPMC E15.

Indian Journal of

Novel Drug Delivery ISSN 0975-5500

Indian Journal of Novel Drug Delivery ISSN 0975-5500