International Journal of Drug Delivery
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The Future of Biosimilars
Get PDFBiosimilars are to Biologic products what generic drugs are to chemical products, a more affordable solution to the increasing drug pricing without sacrificing the quality of the treatment.There is much debate in the health care industry as to whether Biosimilars will deliver on the same success achieved by the generic products, which can amount to up to 80% in some cases. It is my view though that Biosimilars provide a viable path to cost reduction, quality improvement and affordable accessibility to medication. In fact, the introduction of lower costs Biologics as intended by the Biosimilar market will force competition within the therapeutics treatment market that will both exertpricing pressure as well as inspire innovation in the entire ecosystem.
In vitro cytotoxicity, in vivo pharmacokinetic studies and tissue distribution studies of multifunctional citric acid dendrimers using the drug Cytarabine
Get PDFDendrimers are considered the emerging polymeric architectures, known for their well defined molecular-weight, polydispersity, uniformity and high-surface functionality. These nano-architectures are capable of encapsulating low-high molecular-weight drug moieties in their interior or exterior through covalent bonding and host-guest interactions. Further, large surface volume made researchers to implicate dendrimers in biomedical and therapeutic applications. Regardless of the massive applications, sometimes its use is limited because of the cytotoxicity produced. Considering this, the present research is focused on the synthesis and PEGylation of citric acid dendrimers. PEGylation is an act of conjugating polyethylene glycol to dendrimers that completely eliminates the toxicity issues associated with dendrimers and render them biocompatible. Cytarabine was loaded in the dendritic architecture to target specifically the tumor cells. Dendrimers are made tumor specific by incorporating certain agents that get cleaved in tumor environment. Synthesized dendrimers were studied for its effect on acute cytotoxicity, tissue-distributions and pharmacokinetic parameters
Biosynthesis, Characterization and Antibacterial activity of Silver nanoparticles of Excoecaria agallocha L. fruit extract
Get PDFIn this present study, Excoecaria agallocha fruit aqueous extract was used to synthesize Silver Nano Particles (Ag NPs/SNPs) which has proven as eco-friendly, nontoxic, less time consuming and energy saving. The synthesized SNPs were characterized by UV-Visible spectroscopy, FTIR and SEM studies. The SNPs were checked for the antibacterial activity against both Gram positive and Gram negative bacteria. The characterization studies clearly revealed the formation and synthesis of SNPs which also showed the inhibitory activity on the tested bacteria. SNPs of Excoecaria agallocha fruit showed higher zone of inhibition against Micrococcus luteus, Arthrobacter protophormiae, Rhodococcus rhodochrous, Bacillus subtilis, Alcaligens faecalis, Enterobacter aerogenes, Proteus mirabilis and Salmonella enterica when compared to that of standard antibiotic, Streptomycin
Formulations and evaluation of Cyclodextrin complexed Ceadroxil loaded nanosponges
Get PDFCefadroxil (CFD) is a broad spectrum antibiotic that acts against an extensive variety of bacteria, including Gram-positive and Gram-negative bacteria. The major drawback of orally administered drug like cefadroxil is its shorter half life of 1.2 hrs. The goal of the study is to prolong the drug release, producing a desired blood serum level, reduction in drug toxicity and improving the patient compliance by prolonging the dosing intervals. Cyclodextrin-based nanosponges (NS) are a novel class of cross-linked derivatives of cyclodextrins. They have been used to increase the solubility of poorly soluble actives, to protect the labile groups and control the release. This study aimed at formulating complexes of CFDwith three types of β-cyclodextrin NS obtained with different cross-linking ratio (viz. 1:2, 1:4 and 1:8 on molar basis with the cross-linker) to protect the lactone ring from hydrolysis and to prolong the release kinetics of CFD. Crystalline (F1:2, F1:4 and F1:8) and paracrystalline NS formulations were prepared. XRPD, DSC and FTIR studies confirmed the interactions of CFDwith NS. XRPD showed that the crystallinity of CFD decreased after loading. CFD was loaded as much as 21%, 37% and 13% w/w in F1:2 , F1:4 and F1:8, respectively while the paracrystalline NS formulations gave a loading of about 10% w/w or lower. The particle sizes of the loaded NS formulations were between 450 and 600 nm with low polydispersity indices. The zeta potentials were sufficiently high (-20 to -25 mV) to obtain a stable colloidal nanosuspension. The in vitro studies indicated a slow and prolonged CFD release over a period of 24 h. The NS formulations protected the lactone ring of CFD after their incubation in physiological conditions at 37°C for 24 h with a 80% w/w of intact lactone ring when compared to only around 20% w/w of plain CFD
Nanoparticle preparation and characterization of Haruan fish (Channa striata) exctract contains albumin from south Kalimantan with ionic gelation method
Get PDFSnakehead fish (Channa striata) has been reported to be used for wound healing by people in South Borneo because it contains albumin. Snakehead fish extract (Channa striata) has hydrophillic property and poor stability. Nanoparticle technology has been started to be developed as an alternative solution to improve drug delivery profile. The purpose of this study was to determine the formulation that obtained best characterization for nanoparticle. Nanoparticles were prepared by ionic gelation method, that was prepared by doing optimize ratio between snakehead fish extract : chitosan and pH of chitosan solvent.Nanoparticles were characterized using Particle Size Analyzer for particle size and particle size distribution, measurement of entrapment efficiency, determined Zeta potential using Particle Size Analyzer, and observation of particle’s morphology using Transmission Electron Microscope. The result showed that the chosen formula was formula 6 which ratio of extract : chitosan 1:2 with chitosan solvent pH 3, particle size 152.3 nm, polidispersity index 0.778, percentage of entrapment efficiency 51.3961 %, Zeta potential +35.9 mV, and round shape of particles
In vitro and in vivo evaluation of Quetiapine fumarate controlled gastroretentive floating drug delivery system
Get PDFThe aim of the present work was to develop and optimize gastroretentive floating system of Quetiapine fumarate (QF) for the effective treatment of Schizophrenia. The present study was carried out with an objective of preparation and in vivo evaluation of floating tablets of using QF as a model drug using HPMC polymers, Gelucire 43/01 and Polyox WSR 301 to improve oral bioavailability of QF floating tablets by increasing gastric residence time. The tablets were prepared by direct compression method. The effect of polymers concentration and viscosity grades of HPMC on drug release profile was evaluated. The result of in vitro dissolution study showed that the drug release profile could be sustained by increasing the concentration of HPMC K15M and Polyox WSR 301. The optimized formulation (F12) containing HPMC K15M and Polyox WSR301 showed 98.6% drug release at the end of 12h. Changing the viscosity grade of HPMC from K15M to K100M had no significant effect on drug release profile. The optimized formulations (F12) containing sodium bicarbonate 40mg per tablet showed desired buoyancy (floating lag time of about 32seconds and total floating time of >12h). Optimized formulation (F12) followed diffusion controlled zero order kinetics and non-fickian transport of the drug. FTIR and DSC studies revealed the absence of any chemical interaction between drug and polymers used. The best formulation (F12) was selected based on in vitro characteristics and was used in vivo radiographic studies by incorporating BaSO4. These studies revealed that the tablets remained in the stomach for 6h in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered desirable for the absorption window drugs. Studies to evaluate the pharmacokinetics in vivo showed better bioavailability, area under the concentration–time curve, elimination rate constant and half-life than marketed product
Dual buoyant/mucoadhesive macroporous polypropylene microparticles for gastric delivery of repaglinide
Get PDFPreparation and characterization of dual buoyant/mucoadhesive polypropylene microparticles (MPs) loaded with repaglinide (REP) for gastric drug delivery in order to augment the weak mucoadhesion in the stomach.Porous foam powder MPs were prepared using coating polymers with variable permeability (Eudragit L100, Eudragit RSPO) alone or in combination by the soaking method. Thiolated Eudragit L100 (Eudragit L100-SH) was also synthesized and tried in an attempt to enhance the mucoadhesive properties of MPs. All formulae were characterized for their yield, flow properties, particle size, encapsulation efficiency (EE %), morphology, and drug release and its mechanistics. Possible interactions inside MPs matrix were also elucidated using FTIR study. The suitability of the selected formulae for gastroretention was evaluated by in vitro buoyancy and ex-vivo mucoadhesion studies.All REP-loaded MPs demonstrated a passable powder flow, high yield values, promising floatation and mucoadhesion. Encapsulation efficiency % values were nearly tripled upon addition of Eudragit polymers. Compared to the Eudragit free REP loaded foam powder, all formula showed more sustained release features. Eudragit L100-SH was synthesized and confirmed by FTIR. Furthermore, its incorporation, alone or in combination, exhibited a significant increase in mucoadhesion strength compared to the unmodified one.Dual buoyant/mucoadhesive MPs loaded with REP encourage planning for future in-vivo performance studies for the management of diabetes
Formulation and evaluation of once a day matrix tablets of Valsartan
Get PDFThe objective of the research investigation was to design and evaluate the oral once a day matrix tablets of valsartan by using various natural matrix former gums such as separately. Initially natural gums are extracted and purified and their extracts are evaluated for their proximate phyto-chemical studies. Tablets were prepared by wet granulation method. The prepared tablets were further evaluated for physical parameters, In-vitro dissolution, and drug-excipients interactions are also carried out. The FT-IR studies revealed that there was no chemical interaction between drug and excipients. Among all prepared formulations, formulation F-8 exhibited precise controlled release of drug over a prolonged period of 24 hrs. The in- vitro dissolution data obtained for various formulations were fitted into zero order, first order, Higuchi’s and Korsymeyer - Peppas kinetic models. The optimized formulation displayed zero order release kinetics and Korsmeyer and Peppas equation give release pattern with values of (n = 0.9094) indicating non-fickian (or) Anomalous types of diffusion takes place through matrix of Gum Kondagogu. The optimized formulations F-8 was subjected to stability studies for three months at 400C/75%RH as per ICH guidelines and result does not shows any change in physical parameters and in-vitro release studies.
Enhancing Effect of β-Lactoglobulin on the Rate of Cyclosporin Absorption
Get PDFtic The aim of this study was to determine the effects of β-lactoglobulin (β-LG) on the intestinal absorption of cyclosporin A (CsA) in vivo and in vitro. After intraduodenal co-administration of CsA (5 mg/kg) with 150 mg/kg β-LG, Tmax was significantly lower than that of control rats which were given the same dose of CsA without β-LG. Cmax and AUC were significantly increased as compared with the control while T1/2 were not significant. Moreover, a deconvolution method revealed that the rate of CsA absorption was enhanced by β-LG (150 mg/kg) by about 12 times. These results indicate that β-LG significantly enhanced the rate of CsA absorption and the extent of CsA bioavailability in the gut. β-LG did not change the solubility of CsA in vitro, but β-LG increased the apical-to-basolateral permeability clearance of CsA (PScell), with pronounced increase in the permeability of unbound CsA (PSu,cell), across the Caco-2 monolayers in a concentration-dependent manner in vitro. It was thus considered that β-LG-mediated transport of CsA might be a possible mechanism to enhance the intestinal absorption of CsA in vivo
Formulation Development, in-vitro and in-vivo evaluation of novel solid oral dosage form containing Quetiapine nanoparticles.
Get PDFPoorly water soluble drugs such as quetiapine fumarate (QF) offer challenges in developing a solid dosage form such as tablets with adequate bioavailability. The objective of the present work is to develop a solid dosage form for quetiapine nanoparticles in order to increase the saturation solubility, rate of dissolution so that the oral bioavailability is enhanced. Quetiapine fumarate is a BCS class II drug, hence its oral bioavailability is dissolution limited. To enhance the oral bioavailability a nanoparticle formulation of QF was prepared by using high pressure homogenization. The nanosuspension prepared was converted into dry powder by using spray drying. The nanosuspension and spray dried nanoparticles are characterized for particle size, polydispersity index, zeta potential, saturation solubility, drug content, dissolution rate, solid state characterization such as X-ray diffraction(XRD), Differential scanning calorimetry(DSC), infrared(IR), scanning electron microscopy(SEM), transmission electron microscopy(TEM). The spray dried nanoparticles were blended with excipients to convert into solid dosage form such as tablets. The compressed tablets were evaluated for physical parameters, assay and dissolution was compared with the commercial QF formulation. Solid state characterization data showed loss of drug crystallinity after homogenization. The novel dosage form has shown significant increase in the rate of dissolution when compared to microparticle formulation in discriminating medium. In-vivo studies have shown that the rate and extent of absorption of nanoparticle formulation was significantly high when compared to its microparticle formulation when administered in rats