International Journal of Drug Delivery
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Acridone-based acetylcholinesterase inhibitors: synthesis, antioxidant activity and molecular modeling
Get PDFAcridone is a unique naturally occurring alkaloid known to associate with several biological activities. 2,3-dimethoxy-10-methyl-10,8a-dihydroacridin-9(8aH)-one (4) and its precursor 2-((3,4-dimethoxyphenyl)methylamino)benzoic acid (3) were synthesized and investigated for potential antioxidant and inhibitory activity against acetylcholinestrase. The synthetic pathway involves reaction of 2-(methylamino) benzoic acid (1) with 4-chloro-1,2-dimethoxybenzene (2) in presence of CuO and K2CO3 to give the precursor 3. Subsequent, cyclcondensation of 3 with Conc. H2SO4 afforded the anticipated acridone 4. Furthermore, the dimethoxyacridone derivative 4 showed potent antiacetylcholinesterase (ACHE) activity at (100 uM) with IC50 = 9.25 uM that is as potent as the reference drug rivastigmine. Assessment of total antioxidant activity of compounds 3 & 4 in comparison to known standard compounds revealed the following order: α-tocopherol > Acridone 4 > trolox > butylated hydroxyl anisole (BHA) > butylated hydroxyl toluene (BHT) > compound 3. Molecular docking characteristics of 3 & 4 within the active site of AChE (PDB: 1ACJ) co-crystallized with 9-amino-tetrahydroacridine (Tacrine) have been studied. Interestingly, the results revealed comparable binding poses to the co-crystallized ligand and demonstrates good correlation of the binding energy (DG) with the observed IC50-values. This finding suggests that compounds 3 & 4 exhibit good antioxidant effect and inhibition of acetylcholinesterase, which might provide profitable candidates in management of Alzheimer’s disease
Synthesis of Alginate/Nanocellulose bionanocomposite for in vitro delivery of Ampicillin
Get PDFIn this study Ampicillin drug loaded with alginate and nanocellulose film was prepared by solution casting method. Nanocellulose and ampicillin incorporated into alginate to improve both mechanical and swelling property. The formulated ampicillin loaded Alg/NC film gave acceptable physicochemical properties compared with Alg-amp film and was able to deliver the drug in a prolonged release pattern. In vitro drug release showed that alginate, could provide an immediate release of ampicillin with further enhanced nanocellulose, and followed by a sustained release over 500 min of the remaining drug. The present study exhibited a simple and useful approach to systematically design for providing drug release profiles
Preparation of progesterone nanoparticles and evaluation of its effect on the capacitation of Bovine spermatozoa used in the in Vitro Fertilization
Get PDFProgesterone (P) has been reported to affect several sperm functions especially capacitation and acrosome reaction. The main problem of (P) is its low aqueous solubility. So formulation of progesterone nanoparticles (PN) will enhance its solubility. This study was conducted to produce nanosized progesterone (NP) and assess its biocompatibility. Therefore, nine progesterone formulations were prepared and characterized. Data analysis revealed only one formula of P showed nanosized particle (1-100 nm) with an average particle size (95±5 nm), and spherical shape as seen by Transmission Electron Microscope(TEM). Motile spermatozoa were separated from frozen-thawed semen by a swim-up procedure and capacitated in IVF-TALP medium with NP or P or without treatments (control) and incubated for 3h at 38°C and evaluated every 1 hour (h) interval. Ovarian oocytes were matured and fertilized in vitro with frozen-thawed bull sperm capacitated in vitro with NP or P or control (without NP, P) and incubated at 39C in 5% CO2 incubator for 24h and then examined for evidence of fertilization. In conclusion, this study demonstrates that nanosized progesterone is highly efficient for sperm capacitation. In addition to the use of nanosized progesterone in sperm capacitation produces more fertilized oocytes than the progesterone after In Vitro Fertilization (IVF)
Regulatory aspects of medical devices in India
Get PDFToday millions of patients depend on medical device based treatment for the management and diagnose of several diseases. Quality and safety of device is depends upon the regulatory guidelines. Medical device manufacturing in India should be taken seriously due to large population and the potential severity of the consequences of introducing inferior and unsafe products to the market-place. Therefore a law containing adequate guidelines of rules and regulations are required for monitoring the entry of such devices into the use in public health. The regulations define requirements of medical device design, development and manufacture to ensure that products reaching market are safe and effective. Presently in India regulatory body CDSCO is governing regulation for regulation of devices which with time, amendment introducing in the law will provide safety assurance to public health. This review provides a study on different regulatory aspects of medical device implemented in India. The present review discuss about the classification of medical devices and regulations aspects in India
Formulation and evaluation of floating bioadhesive Doxofylline tablets
Get PDFIn the present work, an attempt has been made to develop gastro retentive floating tablets of Doxofylline .HPMC K4M and carbopol were used as controlled release polymers. All the formulations were prepared by direct compression method on 12 station rotary tablet punching machine. The blend of all the formulations showed god flow properties such as angle of repose, bulk density, tapped density. The prepared tablets were shown good post compression parameters and they passed all the quality control evaluation parameters as per I.P limits. FH 5 was the best optimized floating formulation because it released drug completely in 12hrs.It was also observed that the increasing concentration of polymers had a retarding effect on the drug release from the polymer matrices
Formulation And In Vitro/In Vivo Evaluation Of Olmesartan Medoxomil Solid Dispersions Incorporated E/R Trilayer Matrix Tablets By Geomatrix
Get PDFAn attempt has been made to develop and optimize an novel anti hypertensive trilayered controlled release matrix tablets incorporated with Olmesartan medoxomil solid dispersion prepared by direct compression and consisted of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), guar gum, ethyl cellulose. Upper and lower layers are prepared with Carnauba wax, guar gum and sodium CMC. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF14) was described by the Zero-order and Higuchi model. In-vivo bioavailability studies were carried out with the optimized formulation (HF14) and reference standard A fair correlation between the dissolution profile and bioavailability for the optimized formulation was observed. The results indicate that the approach used could lead to a successful development of a trilayer extended release formulation up to 24h. These results also demonstrated that the Olmesartan solid dispersion incorporated trilayer tablets shown more bioavailability because of its conversion from crystalline to amorphous form
Investigations on noval method for the formulation of solid dispersions part- I Formulation, characterization and selection
Get PDFThe solid dispersions of indomethacin with hydrophilic polymers were prepared by lyophilization. The polymers used in the investigation were HPMC, PVP K30, CBR and PLF 127. The solubility and dissolution of indomethacin from prepared lyophilized solid dispersions were investigated in 0.1 N HCl, purified water and USP-NF dissolution media. Out of fifteen lyophilized formulations from F1 to F15, five formulations F2, F5, F8, F12 and F14 showed highest solubility in purified water. Formulation F2, F8 failed to comply with the USP-NF dissolution test for indomethacin capsules. Formulation F14 showed maximum dissolution in the respective dissolution media within 60 min. Sustained drug release was observed for 6 h with formulations F2 and F8 in USP-NF media. The formulations F2, F5, F8, F12 and F14 were characterized by modulated DSC and FT-IR spectroscopy. Some Formulations on stability testing were found physico-chemically stable at accelerated temperature conditions
Synthesis and in vitro drug release studies on substituted polyphosphazene conjugates of lumefantrine.
Get PDFThe present study pertains to the delivery of antimalarial drug (Lumifantrine). In this, polyphosphazene has been used in the synthesis of polyphosphazene-linked conjugates of Lumifantrine. These polymer-linked Conjugates have been synthesized and characterized by modern analytical techniques. The in-vitro drug release of Lumifantrine drug conjugates: p-Amino benzoic acid ester substituted polyphosphazene drug conjugate (15) and Glycine methyl ester substituted polyphosphazene drug conjugate (21) have been found to be 6.00 % and 5.96% (pH 1.2), 88.52% and 79.86% (pH 7.4), respectively. These drug conjugate may prove an effective delivery system for the treatment of malaria
Structural designing of suppressors for autisms spectrum diseases using molecular dynamics sketch
Get PDFIn this paper we are sketching the chemical structure of suppressor drug for autism spectrum disorder using a computational tool. Here we are designing three molecular compounds like Fluoxetine, Risperidone, Melatonin. Structuring the suppressors, sketching the aromatization and bonding of the functional groups with the elements like Oxygen, Nitrogen, halogens. In our work we are using computational algorithm for drawing the structure of suppressor drug. In this paper we are mentioning the autism spectrum suppressor’s molecular formula as well as structural formula
Sustained release formulation of metformin-solid dispersion based on gelucire 50/13- PEG4000: an in vitro study
Get PDFMetformin is a hydrophilic hypoglycemic agent with permeability and short half-life problems which leads to its low bioavailability. Solid dispersion is one of the unique approaches, to improve bioavailability profiles of drugs. The aim of this study was to prepare and evaluate solid dispersions (SDs) of metformin with polyethylene glycol 4000 (PEG 4000) and Gelucire®50/13 in order to increase its permeability and bioavailability. Solid dispersions of Metformin containing various ratios of PEG 4000: Gelucire®50/13 (1:1, 1:2, 2:1, 1:4, 4:1 as Batch A, Batch B, Batch C, Batch D and Batch E) were prepared using solvent evaporation and fusion techniques. The physical mixtures which served as controls were also prepared. The SDs were evaluated using encapsulation efficiency, percentage yield. The formulations were also characterized with FTIR and DSC. The in vitro drug release studies were also evaluated. The results obtained showed that solid dispersion formulations at pH, 1.2 and 7.4 demonstrated higher release rates than the pure drug. The SDs showed high drug release rates and encapsulation efficiency (% EE) although Batch C containing PEG 4000 and Gelucire 50/13 in the ratio of 2:1 appeared as the batch with most % EE, drug release with broad melting peak. The release rate of metformin increased with increasing amount of PEG 4000. Batch C, SDs containing PEG 4000 and Gelucire 50/13 in the ratio of 2:1 were found to be the most optimized batch with enhanced encapsulation efficiency, most drug release and therefore, improved permeability and bioavailability of metformin