Publications (21)27.72 Total impact
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Article: Enhanced intestinal absorption and bioavailability of raloxifene hydrochloride via lyophilized solid lipid nanoparticles
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ABSTRACT: The current oral therapy with raloxifene hydrochloride (RXH) is less effective due to its poor bioavailability (only 2%). Henceforth, an attempt was made to investigate the utility of triglyceride (trimyristin, tripalmitin and tristearin) based solid lipid nanoparticles (SLNs) for improved oral delivery of RXH. The SLN formulations prepared were evaluated for particle size, zeta potential and % entrapment and the optimized formulation was lyophilized. Solid state characterization studies unravel the transformation of RXH to amorphous or molecular state from the native crystalline form. Further the in situ perfusion studies carried out in rat intestine reveal the potential of SLN for enhanced permeation of raloxifene HCl across gastrointestinal barrier. To derive the conclusions, in vivo pharmacokinetic study was conducted in rats to assess the bioavailability of RXH from SLN formulation compared to drug suspension. Overall a twofold increase in bioavailability with SLN formulations confer their potential for improved oral delivery of RXH.Advanced Powder Technology 10/2012; · 1.61 Impact Factor -
Article: In situ absorption and relative bioavailability studies of zaleplon loaded self-nanoemulsifying powders.
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ABSTRACT: Self-nanoemulsifying drug delivery systems (SNEDDSs) offer potential as suitable carriers for improved oral delivery of poorly soluble and low bioavailable drugs. To derive self-nanoemulsifying powders (SNEPs), the optimized Z-SNEDDS formulation was adsorbed onto different carriers and based on micromeritics the formulation loaded onto neusilin US2 (SNEP-N) was selected for further characterization. The solid-state characterization (scanning electron microscopy, differential scanning calorimetry and powder X-ray diffraction) studies unravel the transformation of native crystalline state to amorphous and/or molecular state. The higher predictive effective permeability coefficient and fraction absorbed in humans extrapolated from in situ single-pass intestinal absorption study data in rats provide an insight on the potential of SNEPs for augment in absorption across gastrointestinal barrier. Overall a 3.5-fold enhancement in the extent of absorption of zaleplon from SNEP-N formulation proves the feasibility of SNEPs formulation for improved oral delivery of zaleplon.Journal of Microencapsulation 08/2012; · 1.55 Impact Factor -
Article: Proliposome powders for enhanced intestinal absorption and bioavailability of raloxifene hydrochloride: effect of surface charge.
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ABSTRACT: The primary goal of the present study was to investigate the combined prospective of proliposomes and surface charge for the improved oral delivery of raloxifene hydrochloride (RXH). Keeping this objective, the present systematic study was focused to formulate proliposomes by varying the ratio of hydrogenated soyphosphatidylcholine and cholesterol. Furthermore, to assess the role of surface charge on improved absorption of RXH, anionic and cationic vesicles were prepared using dicetyl phosphate and stearylamine, respectively. The formulations were characterized for size, zeta potential and entrapment efficiency. The improved dissolution characteristics assessed from dissolution efficiency, mean dissolution rate were higher for proliposome formulations. The solid state characterization studies indicate the transformation of native crystalline form of the drug to amorphous and/or molecular state. The higher effective permeability coefficient and fraction absorbed in humans extrapolated from in situ single-pass intestinal absorption study data in rats provide an insight on the potential of proliposomes and cationic surface charge for augment in absorption across gastro intestinal barrier. To draw the conclusions, in vivo pharmacokinetic study carried out in rats indicate a threefold enhancement in the rate and extent of absorption of RXH from cationic proliposome formulation which unfurl the potential of proliposomes and role of cationic charge for improved oral delivery of RXH.Drug Development and Industrial Pharmacy 03/2012; · 1.49 Impact Factor -
Article: Bioavailability enhancement of zaleplon via proliposomes: Role of surface chargeKarthik Y. Janga1, Raju Jukanti, , Ashok Velpula1, Sharath Sunkavalli1, Suresh Bandari, Prabhakar Kandadi, Prabhakar Reddy VeerareddyDepartment of Pharmaceutics, St. Peter’s Institute of Pharmaceutical Sciences, Warangal, India
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ABSTRACT: The present systematic study focused to investigate the combined advantage of proliposomes and surface charge for improved oral delivery of zaleplon. The zaleplon loaded proliposomes were prepared using hydrogenated soyphosphatidylcholine (HSPC) and cholesterol (CHOL) in varying ratios, and the optimized formulation was tailored with dicetyl phosphate and stearylamine to obtain negative and positive charged vesicles, respectively. The formulations were characterized for micromeritics, size, zeta potential, and entrapment efficiency. Further, in vitro release and dissolution study carried out provide an insight on the stability and enhanced dissolution of zaleplon from proliposome formulations. The solid state characterization (SEM, DSC, and PXRD) studies unravel the transformation of zaleplon to amorphous or molecular state from the native crystalline form. To depict the conclusions, in situ single-pass perfusion and bioavailability studies were carried out in rats. The significant increase in effective permeability coefficient (Peff) and rate and extent of absorption from cationic vesicles indicate the importance of surface charge for effective uptake across the gastrointestinal tract. Overall a two- to fivefold enhancement in bioavailability in comparison with control confers the potential of proliposomes as suitable carriers for improved oral delivery of zaleplon.European Journal of Pharmaceutics and Biopharmaceutics 02/2012; 80(2):347-357. · 4.27 Impact Factor -
Article: Bioavailability enhancement of zaleplon via proliposomes: Role of surface charge.
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ABSTRACT: The present systematic study focused to investigate the combined advantage of proliposomes and surface charge for improved oral delivery of zaleplon. The zaleplon loaded proliposomes were prepared using hydrogenated soyphosphatidylcholine (HSPC) and cholesterol (CHOL) in varying ratios, and the optimized formulation was tailored with dicetyl phosphate and stearylamine to obtain negative and positive charged vesicles, respectively. The formulations were characterized for micromeritics, size, zeta potential, and entrapment efficiency. Further, in vitro release and dissolution study carried out provide an insight on the stability and enhanced dissolution of zaleplon from proliposome formulations. The solid state characterization (SEM, DSC, and PXRD) studies unravel the transformation of zaleplon to amorphous or molecular state from the native crystalline form. To depict the conclusions, in situ single-pass perfusion and bioavailability studies were carried out in rats. The significant increase in effective permeability coefficient (Peff) and rate and extent of absorption from cationic vesicles indicate the importance of surface charge for effective uptake across the gastrointestinal tract. Overall a two- to fivefold enhancement in bioavailability in comparison with control confers the potential of proliposomes as suitable carriers for improved oral delivery of zaleplon.European journal of pharmaceutics and biopharmaceutics: official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V 02/2012; 80(2):347-57. · 3.15 Impact Factor -
Article: Improved Ex Vivo Transcutaneous Permeation of Diclofenac from Solid Lipid Nanoparticles in the Presence of Novel Long-Chain Alkyl Esters of PABA
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ABSTRACT: The current study aimed to evaluate long-chain alkyl esters of p-amino benzoic acid (PABA) as possible new class of permeation enhancers. In this study we have synthesized long-chain alkyl esters of PABA (decyl, dodecyl, and tetradecyl) by a novel and facile method in our laboratory. The PABA derivatives were incorporated into solid lipid nanoparticles and characterized for size, zeta potential and entrapment efficiency. In vitro permeation study was carried out using rat abdominal skin and permeation enhancement was assessed from the permeation parameters (flux, permeability coefficient, and enhancement ratio). Among the formulations tested, Dodecyl PABA containing solid lipid nanoparticles (SLN) has shown a significant enhancement in the permeation of diclofenac compared to control and other PABA derivatives containing solid lipid nanoparticles. The increase in permeation parameters clearly indicates the potential of PABA derivatives as a novel amphiphile that can be explored as a new class of permeation enhancers in topical drug delivery.Journal of Dispersion Science and Technology 08/2011; 32(8):1158-1164. · 0.56 Impact Factor -
Article: Transcorneal Permeation of Ciprofloxacin Liposomes: Effect of Surface Charge and Nonionic Surfactants
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ABSTRACT: The success of an ocular delivery system is dependent on the reduction in the precorneal loss of the drug by prolonging the contact time and increasing permeability across the corneal barrier which makes the drug more bioavailable to the ocular tissue. The current investigation aimed to improve the transcorneal permeation of ciprofloxacin hydrochloride by loading into liposomes. The liposomes were prepared and investigated the role of surface charge and nonionic surfactants on the permeation of ciprofloxacin from liposomes across isolated corneal membrane. Among the formulations tested, the liposomes containing stearylamine and polysorbate 80 exhibited higher transcorneal permeation compared to other formulations. A two fold increase in the flux and enhancement ratio was observed for these formulations. The corneal hydration levels tested for the liposomal formulations were within the limits. The data reveals the potential of positive charge and nonionic surfactants in successful delivery of ciprofloxacin across the corneal barrier.Journal of Dispersion Science and Technology 07/2011; 32(7):935-942. · 0.56 Impact Factor -
Article: Drug targeting to inflammation: studies on antioxidant surface loaded diclofenac liposomes.
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ABSTRACT: Inflammation is associated with enhanced vascular permeability, production of inflammatory markers and over production of reactive oxygen species (ROS) with depletion of endogenous antioxidants. Several drug targeting approaches to inflammation taking clues from these events have been evolved. Surprisingly, a drug targeting approach utilizing abundant oxidative stress at inflammatory site has not been followed. Antioxidant surface loaded liposomes might preferentially localize at inflammatory sites via redox interaction where at high level of ROS exist. The present study was focused to investigate the role of antioxidant as a targeting ligand on the surface of liposome employing rat granuloma air pouch model of inflammation. We developed conventional and antioxidant loaded diclofenac (DFS) liposomes (co-enzyme Q10 and ascorbyl palmitate) for i.v. administration and characterized for vesicle size, zeta potential and percent entrapment. In vivo drug targeting studies showed an increase in AUC, therapeutic availability of DFS in air pouch fluid (APF) and APF/serum DFS concentration ratios from antioxidant loaded liposomes compared to conventional liposomes and drug solution. The promising results suggest the role of antioxidant as a possible ligand in drug targeting to a site where at abundant ROS exist.International journal of pharmaceutics 05/2011; 414(1-2):179-85. · 2.96 Impact Factor -
Article: Transdermal Delivery of Acyclovir Sodium Via Carbopol Gels: Role of Chemical Permeation Enhancers
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ABSTRACT: The effective management of the cutaneous herpes simplex virus infections with acyclovir sodium (ACV) is limited due to reduced availability of ACV at the basal epidermis. The present research focused to improve the transcutaneous permeation of ACV from carbopol gels with different chemical permeation enhancers (dimethylsulfoxide, dlimonene, sodium taurodeoxycholate). The ex-vivo permeation was carried out using excised rat abdominal skin. The extent of ACV accumulated in the rat skin layers was also estimated and found to be higher with gel based formulations compared to reference formulation. Further, the irritancy test and histological studies were carried out to understand the mechanism of ACV permeation across stratum corneum. The improvement in the transcutaneous permeation assessed from steady state flux, permeability coefficient and enhancement ratio were significantly enhanced with gel formulations compared to reference formulation. In conclusion, research findings reveal the potential of carbopol gels for maximizing the therapeutic benefit in herpes virus infections.Letters in Drug Design & Discovery 04/2011; 8(4):381-389. · 0.87 Impact Factor -
Article: Preparation and evaluation of mucoadhesive cefdinir microcapsules.
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ABSTRACT: The mucoadhesive microcapsules were prepared by using various concentrations of three different mucoadhesive polymers, namely, chitosan, Carbopol 934P, and methyl cellulose as wall materials and cefdinir as the core material employing orificeionic gelation method. The prepared microcapsules were characterized by scanning electron microscope (SEM) and Fourier transform infrared spectrometry (FT-IR). The prepared microcapsules were found to be spherical with particle size ranging from 765±20 to 985±10 μm and encapsulation efficiencies in the range of 55%-92%. The formulation containing Carbopol 934P as mucoadhesive polymer was found to be best with particle size 946±10 μm. The ex vivo wash-off test showed that the mucoadhesion after 1 h was 80% and the in vitro drug release was extended for more than 12 h. FT-IR spectra indicate that there was no interaction between drug and the polymers used in the formulation. Cefdinir is better absorbed from the upper part of the gastrointestinal tract, it suffers from low oral bioavailability (20-30%), shorter biological half-life (1-2 h), and less transit time. Thus, it can be concluded that microcapsules prepared using Carbopol 934P have promising properties for use as mucoadhesive carrier to increase the residence time of cefdinir.Journal of Advanced Pharmaceutical Technology & Research 04/2011; 2(2):115-20. -
Article: Enhanced bioavailability of exemestane via proliposomes based transdermal delivery.
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ABSTRACT: Exemestane, a novel steroidal aromatase inactivator used in the treatment of advanced breast cancer has limited bioavailability (42%) due to poor solubility, extensive first-pass metabolism, and also the absorption is dependent on formulation type and food. The present study is aimed to evaluate the feasibility of proliposomes for transdermal delivery of exemestane. The prepared proliposomes were characterized for size, zeta potential, and entrapment efficiency. The size of the vesicles was found to be between 440 and 700 nm with high entrapment efficiency for the formulation containing greater amounts of phosphatidylcholine. Differential scanning calorimetry and Fourier transform infrared studies were performed to understand the phase transition behavior and mechanism for skin permeation, respectively. The drug release across cellophane membrane follows zero-order kinetics by diffusion. Ex vivo permeation enhancement assessed from flux, permeability coefficient, and enhancement ratio were significantly higher for proliposome gels compared with control. A significant improvement in the bioavailability (2.4-fold) was observed from optimized proliposome gel compared with control (oral suspension). The stability data reveal that the formulations are more stable when stored at 4°C. In conclusion, proliposomal gels offer potential and prove to be efficient carriers for improved and sustained transdermal delivery of exemestane.Journal of Pharmaceutical Sciences 03/2011; 100(8):3208-22. · 3.06 Impact Factor -
Article: Colon-Specific Microparticles of Piroxicam: Formulation and Optimization Using 3 2 Factorial Design
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ABSTRACT: The aim of the present study was to prepare and evaluate colon-specific microparticles of piroxicamby oil/water emulsion solvent evaporation method. A 32 factorial design as employed to study the combined influence of two independent variables amount of piroxicam (X1) and amount of eudragit S-100 (X2) on dependent variables, encapsulation efficacy (Y1), percentage cumulativedrug release at the fifth hour (Y2), and percentage cumulative drug release at the tenth hour (Y). The microparticles were evaluated for micromeritic properties and drug release studies. Drug–polymer interaction was determined by differential scanning calorimeter, x-ray powder diffraction. The surface morphology and spherocity was studied by scanning electron microscopy. The developed piroxicam microparticles showed desired colon-specific delivery.Journal of Dispersion Science and Technology 01/2011; 32(10):1396-1403. · 0.56 Impact Factor -
Article: Biodistribution of ascorbyl palmitate loaded doxorubicin pegylated liposomes in solid tumor bearing mice.
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ABSTRACT: The aim of this study is to develop ascorbyl palmitate (ASP) loaded doxorubicin (DOX) pegylated liposomes and to evaluate their targeting potential to tumor. We have prepared conventional (DL), pegylated DOX liposomes with (SDL) and without ascorbyl palmitate (SDL-A). The vesicle size in all the formulations was within the range 105-120 nm and in vitro release studies in serum confirmed the stability of the liposomes. Biodistribution studies carried out in Ehrlich ascites tumor bearing mice indicate higher area under the curve for SDL and SDL-A liposomes compared to DL and plain drug solution. Drug targeting index assessed from tumor-to-serum concentration ratio and therapeutic availability of DOX in tumor tissue was also significantly higher for pegylated liposomes. In conclusion, biodistribution study reveals that the presence of ascorbyl palmitate alters the distribution pattern of liposomes and paves way for better drug targeting.Journal of Microencapsulation 01/2011; 28(2):142-9. · 1.55 Impact Factor -
Article: Formulation and Evaluation of Gastroretentive Dosage Form of Ofloxacin
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ABSTRACT: Abstract: The aim of the present investigation was to develop and evaluate gastroretentive drug delivery tablets (GRDDTs) of ofloxacin using different polymers such as HPMC K4M, HPMC K15M, Polyethylene oxide WSR 303, Carbopol 971P, Xanthan Gum in different ratios for local action in gastric region to eradicate Helicobacter pylori infection. The GRDDTs were prepared by wet granulation method and evaluated for physical characteristics such as hardness, thickness, friability, drug content and floating properties. The optimized formula F4 showed better sustained drug release and which also had good floating properties and fitted best to be Korsmeyer-Peppas model with R2 value of 0.9848. As the n value for the Korsmeyer- Peppas model was found be less than 0.45 it follows Fickian diffusion mechanism. FT-IR result showed that there is no drug excipient interaction. In vivo radiographic studies were conducted with BaSO4 loaded tablets to examine the increased gastric residence time of the prepared tablets. The study revealed that the tablet remained in the stomach for 300±10min which indicates the increase in the gastric residence time for the effective localized action of the ofloxacin in the treatment of Helicobacter pylori caused peptic ulcer.Stamford Journal of Pharmaceutical Sciences 01/2011; 4(1):9-18. -
Article: Solubility enhancement and physicochemical characterization of carvedilol solid dispersion with Gelucire 50/13.
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ABSTRACT: The objective of the study was enhancement of dissolution of poorly soluble carvedilol by solid dispersions (SDs) with Gelucire 50/13 using solvent evaporation method. The solubility of carvedilol showed linear increase with increasing concentrations of Gelucire indicating A(L) type solubility diagrams. SDs characterized for physicochemical characteristics using differential scanning calorimetry and X-ray diffractometry revealed transformation of crystalline form of drug to amorphous form which was confirmed by scanning electron micrographs. Further fourier transform infrared spectroscopy results suggested there is no drug carrier interaction. From the dissolution parameters such as mean dissolution time, dissolution efficiency and drug release rate, improved dissolution characteristics for SDs were observed compared with physical mixture and pure drug. Thus SDs of carvedilol in Gelucire 50/13 showed enhanced solubility and dissolution rate compared to pure drug.Archives of Pharmacal Research 01/2011; 34(1):51-7. · 1.59 Impact Factor -
Article: Formulation and In Vitro Evaluation of Pulsatile Colon DrugDelivery System of Piroxicam using 32 Factorial design
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ABSTRACT: The aim of the present investigation was to develop colon specific double cross linked alginatechitosan blend gel beads for pulsatile release. A 32 factorial design was employed to study the influence of two independent variables amount of piroxicam (X1), amount of chitosan (X2) on dependent variables, encapsulation efficacy (YEE), amount of drug release at 5th hour (Y5) and amount of drug release at 6th hour (Y6). The prepared colon specific pulsatile beads were evaluated for particle size and invitro drug release studies. Drug polymer interaction studies were determined by fourier transform infrared (FTIR) spectroscopy. The surface characteristics and morphology was determined by scanning electron microscopy (SEM). The check point batch was prepared and the contour and 3D plots were also presented. It was concluded that the desired colon specific pulsatile release was obtained with alginate-chitosan blend gel double cross linked beads.Der Pharmacia Lettre. 01/2010; 2:177-188. -
Article: Formulation and Pharmacodynamic Evaluation of Meloxicam Liquisolid Compacts
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ABSTRACT: SUMMARY. The purpose of this study was to improve the meloxicam dissolution rate through its formulation into liquisolid compacts and then to evaluate the in vitro and in vivo performance of the prepared liquisolid compacts. Dissolution efficiency, mean dissolution time and relative dissolution rate of liquisolid compacts were calculated and compared to marketed formulation. The degree of interaction between the ME and excipients was studied by differential scanning calorimetry and X-ray diffraction were used and results revealed that, there was a loss of meloxicam crystallanity upon liquisolid formulation and almost molecularly dispersed state, which contributed to the enhanced drug dissolution properties. The optimized liquisolid compact showed higher dissolution rates and dissolution efficiency compared to commercial product. The analgesic and anti inflammatory response of optimized liquisolid compact in Swiss albino mice and Wistar rats was found to be superior compared to the marketed formulation.Latin American Journal of Pharmacy. 01/2010; 29:1303-10. -
Conference Proceeding: Optimization of Colon Specific Eudragit S-100 microspheres of piroxicam using 32 factorial design
IPC-2009, Nirma University of Science and Technology, Ahmedabad, India.; 01/2009 -
Article: Rapid and simple liquid chromatography tandem mass spectrometry method for the quantification of zidovudine in rat plasma.
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ABSTRACT: A high-performance liquid chromatography/electrospray ionization tandem mass spectrometry method was developed and validated for the quantification of zidovudine in rat plasma. Following solid-phase extraction, the analytes were separated using an isocratic mobile phase on a reverse phase column and analyzed by MS/MS in the multiple reaction monitoring mode using the respective [M+H]+ ions, m/z 268/127 for zidovudine and m/z 230/112 for the internal standard. The method exhibited a linear dynamic range of 5-500 ng/mL for zidovudine in rat plasma. The lower limit of quantification was 5 ng/mL with a relative standard deviation of less than 8%. Acceptable precision and accuracy were obtained for concentrations over the standard curve range. A run time of 1.5 min for each sample made it possible to analyze more than 400 plasma samples per day. The validated method was applied for pharmacokinetic studies of the novel drug delivery systems of zidovudine in rats.Biomedical Chromatography 02/2008; 22(1):20-7. · 1.97 Impact Factor -
Article: HPLC quantification of the HIV-1 protease inhibitor saquinavir in brain and testis of mice.
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ABSTRACT: A rapid, reliable HPLC method with UV detection (240 nm) was developed and validated for quantitation of saquinavir in mice brain and testis. Saquinavir and the internal standard were isolated from homogenized tissue matrices using liquid-liquid extraction procedure and were then analyzed using an isocratic mobile phase by reversed-phase liquid chromatography. The lower limit of quantification was 50 ng/g for both brain and testis. A linear dynamic range of 50-5000 ng/g for both brain and testis was established. This HPLC method was validated with between-batch precision of 0.5-4.4 and 1.5-5.5% for brain and testis, respectively. The between-batch accuracy was 94.7-105.9% and 97.5-105.0% for brain and testis, respectively. The present method was applied for tissue distribution studies of the novel drug delivery systems of saquinavir in mice.Biomedical Chromatography 11/2006; 20(10):1028-32. · 1.97 Impact Factor
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Institutions
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2011–2012
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St. Peter's Institute Of Pharmaceutical Sciences
Warangal, State of Andhra Pradesh, India -
Kakatiya University
Warangal, State of Andhra Pradesh, India
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