Search

Celecoxib exhibits poor flow properties and compressibility. Spherical crystallization of celecoxib was carried out using the solvent change method. An acetone:dichloromethane (DCM):water system was used where DCM acted as a bridging liquid and acetone and water as good and bad solvent, respectively. Hydroxypropylmethylcellulose (HPMC) was used to impart strength and sphericity to the agglomerates. The effect of amount of bridging liquid and speed of agitation was studied using 32 factorial design. Primary properties of the agglomerates were evaluated by infrared spectroscopy, powder X-ray diffraction, and differential scanning calorimetry. The effect of variables on micromeritic, mechanical, compressional, and dissolution behavior was evaluated by response surface methodology. Particle size, bulk density, mean yield pressure (MYP), and drug release were found to be significantly affected by either of the two variables. Interaction of variables significantly affected the MYP.

Objective: Suicide is known to be a phenomenon in low-, middle-, and high-income countries and occurs in all sociodemographic groups. It ranges from acute to fatal lethal attempts which occur in the context of a social crisis. Deliberate self-poisoning for suicide is a growing public health concern with frequent emergency department admissions. An epidemiological surveillance is essential for every region to understand the pattern, underlying psychological factors, and the scope of preventive measures.Methods: The 2-year retrospective study describes the epidemiology and influencing factors of suicides by self-poisoning in patients admitted to a Government Hospital and a Teaching Hospital in Pune, Maharashtra, from January 1, 2014 to December 31, 2015.Result: Out of 1010 poisoning cases reported, 539 were suicidal self-poisoning. Significantly males more than females were brought to the hospitals due to deliberate self-poisoning (1:0.86, χ2=38.05; p

Objective: The present study aims to determine the pattern of antibiotic utilization at the surgery department of a tertiary care hospital.Method: A prospective observational study was conducted over a period of 6 months period in surgical ward at Bharti Hospital and Research Centre, Pune, a 1000 bedded teaching hospital. Patients above 18 years and receiving antibiotic therapy pre and post-surgery were included in the study.Results:160 patients with surgical operations were included in the study.The disease spectrum was classified into respective system-wise surgical procedures of which 49.37% cases are skin & soft tissue infections, 25.62% cases of general surgical procedure, 12.5% cases of gastrointestinal surgical procedure, 11.25% cases of urinary system and 1.25% case of head neck system. 20.62% of the study patients had hernia, 18.12% patients had cellulitis, 16.87% patients had diabetic foot ulcer, 16.25% patients had abscess, and 10.62% patients had appendicitis and cholelithiasis. In this study, it was found that 471 antibiotics were used in total of 160 patients, among which highest group of antibiotics prescribed were third generation Cephalosporin (28.23%) followed by Penicillins (23.56%). The most frequently prescribed antibiotics were Metronidazole − 19.74% among the Nitroimidazoles followed by Ceftriaxone − 19.53% of the class Cephalosporins.Conclusion: The rate of prescribing of broad-spectrum antibiotics has increased demonstrably which may result in development of bacterial resistance; however development of guidelines for antibiotic prescription and use of appropriate drugs for the diseases can minimize the unfavourable use of antibiotics and cost of healthcare.

The progress in the development of DPI technology has boosted the use of sensitive drug molecules for lung diseases. However, delivery of these molecules from conventional DPI to the active site still poses a challenge with respect to deposition efficiency in the lung. At same time, serious systemic side effects of drugs have become a cause for concern. The developed budesonide loaded biopolymer based controlled release DPI had shown maximum in vitro lung deposition with least toxicity. The subject of present study, lactose-free budesonide loaded biopolymer based DPI, further corroborates the great potential of antiasthmatic drugs. This technology is expected to revolutionize the approaches towards enhanced therapeutic delivery of prospective drugs.

The natural flavonoid fisetin has shown anticancer properties but its in vivo administration remains challenging due its poor aqueous solubility and extensive in vivo metabolism. This juncture demands an effective, controlled release and safe formulation of fisetin would be a significant advance for the treatment of cancer.Nanocochleates are unique lipid-based supramolecular assemblies composed of a negatively charged phospholipid and a divalent cation. The aim was to develop and evaluate fisetin-loaded nanocochleates to improve its therapeutic efficacy. Using the trapping method, fisetin-loaded dimyristoylphosphatidylcholine liposomal vesicles were converted into nanocochleates by the action of Ca(2+) ions. These nanocochleates were further evaluated for physicochemical, in vitro anticancer and haemolysis, pharmacokinetics and tissue distribution study in mice.Stable rolled-up layers as well as elongated structure of nanocochleates possessing particle size and encapsulation efficiency (EE) of 275 + 4 nm and 84.31 ± 2.52%, respectively were obtained. Nanocochleates demonstrated safety and a sustained release of fisetin at physiological pH. A 1.3-fold improvement in vitro anticancer towards human breast cancer MCF-7 cells was observed. Pharmacokinetics studies in mice revealed that nanocochleates injected intraperitonially showed a 141-fold higher relative bioavailability. Moreover, a low tissue distribution was observed.Developed nanocochleates markedly improved anticancer efficacy, bioavailability and safety of fisetin. The nanocochleates technology would facilitate the administration of this flavonoid in the clinical setting.In this research article, we focused on lipid-based supramolecular assembly 'nanocochleates' composed of negatively charged phospholipids and divalent cation as drug carrier for systemic delivery system and discussed their formulations, optimisation, characterization, in vitro and in vivo performance.

The aim of present study was to develop and characterize polymeric micelle (PMs) of anticancer drug, Capecitabine (CTB). Preliminary trial batches were employed to screen the significant formulation and process variables of CTB loaded polymeric micelles by Quality-by-Design (QbD) approach. Eight variables were screened and the results showed Eudragit S 100 and HP β Cyclodextrin (HP β-CD) to be the most significant factors influencing mean particle size and zeta potential of the polymeric micelle formulation. The main effects plot depicted that all the independent variables had a statistically significant effect on the response variables. The selected batch was then studied for different characterization parameters and for invitro cytotoxicity studies.

A 63-year-old woman, after 5 years of resection of craniopharyngioma, developed recurrence of tumor with acute onset of psychotic symptoms. After 4 years of resection of craniopharyngioma, the patient presented with psychotic symptoms of varied delusion of reference, persecution, black magic and occasional auditory hallucinations. On physical examination, she showed no neurological deficit. Her blood investigations were at normal levels. Her recent magnetic resonance imaging brain scan showed large cystic lesion supposed to be a recurrent mass in sellar and suprasellar regions. After 2 months of antipsychotic treatment, her delusions and hallucinations were much decreased to extent that now she can do some household work. Her psychosis was controlled while she awaits neurosurgical intervention for recurrent craniopharyngioma. Acute psychosis is rarely found in elderly people and after few years of craniotomy for craniopharyngioma resection. So, the psychosis can be associated with the recurrence of craniopharyngioma. Such psychosis needs surgical intervention for primary cause.

Introduction Various shortcomings of the available methods of extraction of plumbagin from Plumbago zeylanica using non-edible organic solvents coupled with the poor aqueous solubility and low bioavailability called for extracting plumbagin in a water soluble form via a single step technique using hydrophilic lipid Gelucire 44/14. Methods Gelucire extract of P. zeylanica (GPZ) was prepared and evaluated for extraction efficiency, High-performance thin layer chromatography (HPTLC) and thermal analysis. In vitro intestinal absorption and bioavailability of plumbagin from GPZ in comparison with that of aqueous (APZ), ethanolic extract (EPZ) and standard plumbagin studied using non-everted rat intestinal sac model. Results The GPZ showed significantly higher extraction efficiency (3.24 ± 0.12% w/w) compared to ethanolic (EPZ) and aqueous (APZ) extraction, 2.48 ± 0.16% w/w and 0.07 ± 0.02% w/w respectively. GPZ displayed significantly higher Q 30min (cumulative percentage absorption of plumbagin in 30 min) and lower t 40% (time required for 40% w/w drug absorption). The flux and apparent permeability coefficient in duodenum and ileum were 2, 3 and 6 fold higher than EPZ, standard plumbagin and APZ respectively. Discussion Improved therapeutic efficacy of plumbagin may be due to the micellar solubilization and consequent enhanced partitioning of plumbagin through intestinal by Gelucire which was reflected in the in vivo anti-inflammatory study conducted in rats. Conclusion Thus extraction using Gelucire can be proclaimed as an efficient, economic and solvent-free technique for extraction of plumbagin and can be utilized for various clinically important water insoluble phytoconstituents in order to improve their biopharmaceutical properties.

The aim of this study was to develop photostable gastro retentive formulation for nifedipine loading into low-density polypropylene microporous particles (Accurel MP 1000®) by a solvent evaporation technique using the 3² factorial design. Yield, drug loading, surface topography, thermal properties, crystal characteristics, photostability and in vitro drug release were studied. Optimized microparticles formulated into a capsule were evaluated for the dissolution study and compared with marketed formulation. Higher values of T(₅₀%), time required for 50% degradation of drug with threefold and 1.5-fold decrease in degradation rate constant (K) under UV and fluorescent lamp were observed for the microparticles, respectively, as compared to pure nifedipine indicated remarkable improved photostability. Microparticles showed good floating ability in 0.1N HCl with initial burst release (16-29%) followed by the zero-order drug release up to 8 h. The capsule formulation followed the ideal modified release pattern.

Niosomal delivery can prove an alternative to improve the poor skin penetration and residence of the topical antifungal drugs that account for the long treatment regimes in cutaneous mycosis.To investigate niosomes as carriers for dermal delivery of ciclopirox olamine (CPO), a broad spectrum antifungal drug.Niosomes were prepared by ethanol injection method using Span 60, cholesterol, diacetyl phosphate according to 3(2) factorial design and evaluated for physicochemical parameters, in vitro and ex vivo deposition in skin and stability study.Unilamellar CPO niosomes of size 170-280 nm, entrapment efficiency 38-68%, and sufficient electrokinetic stability were obtained. Percent drug deposition in artificial membrane varied from 12.75 to 92.74. Deposition of CPO into rat skin from niosomal dispersion and its gel was significantly higher than that of plain CPO solution and its marketed product. Obtained niosomes possessed sufficient stability on storage.Increasing amounts of Span 60 and cholesterol increase the vesicle size probably because of entrapment of CPO-ionized molecules in the aqueous compartment and interaction of its unionized counterpart with the bilayer constituents leading to increase in bilayer thickness. Consequently, the percent entrapment efficiency also increased. However, increasing Span 60 levels decreased the in vitro percent drug deposition. This might be attributed to the larger size of vesicles produced by high amounts of surfactant that showed poor deposition. The optimized batch possessed sufficient stability.The results of this investigation suggest that niosomes are promising tools for cutaneous retention of CPO.

The objective of the investigation was to study the effect of bromhexine hydrochloride (BXH) content and agglomerate size on mechanical, compressional and drug release properties of agglomerates prepared by crystallo-co-agglomeration (CCA). Studies on optimized batches of agglomerates (BXT1 and BXT2) prepared by CCA have showed adequate sphericity and strength required for efficient tabletting. Trend of strength reduction with a decrease in the size of agglomerates was noted for both batches, irrespective of drug loading. However, an increase in mean yield pressure (14.189 to 19.481) with an increase in size was observed for BXT2 having BXH-talc (1:15.7). Surprisingly, improvement in tensile strength was demonstrated by compacts prepared from BXT2, due to high BXH load, whereas BXT1, having a low amount of BXH (BXH-talc, 1:24), showed low tensile strength. Consequently, increased tensile strength was reflected in extended drug release from BXT2 compacts (Higuchi model, R2 = 0.9506 to 0.9981). Thus, it can be concluded that interparticulate bridges formed by BXH and agglomerate size affect their mechanical, compressional and drug release properties., Cilj rada bio je praćenje utjecaja sadržaja bromheksidin hidroklorida (BXH) i veličine aglomerata na mehanička svojstva, kompresivnost i oslobađanje ljekovite tvari iz aglomerata pripravljenih kristalokoaglomeracijom (CCA). Optimizirani pripravci aglomerata (BXT1 i BXT2) pripravljeni CCA metodom pokazuju adekvatnu sferičnost i čvrstoću potrebnu za učinkovito tabletiranje. U oba pripravka se smanjenjem veličine aglomerata smanjivala i čvrstoća, neovisno o količini ljekovite tvari. Međutim, povećanje prosječnog tlaka s povećanjem veličine čestica primijećeno je u pripravku BXT2 s omjerom BXH-talk 1:15,7. Iznenađuje da su kompakti pripravljeni iz BXT2, s visokim sadržajem BXH, imali veću vlačnu čvrstoću, dok su BXT1 s niskim sadržajem BXH (BXH-talk, 1:24) imali manju čvrstoću. Veća vlačna čvrstoća imala je za posljedicu produljeno oslobađanje ljekovite tvari iz BXT2 (Higuchijev model, R2 = 0,9506 do 0,9981). Može se zaključiti da mostovi među česticama BXH i veličina aglomerata utječu na njihova mehanička i kompresivna svojstva te na oslobađanje ljekovite tvari.

The objective of the investigation was to study the effect of bromhexine hydrochloride (BXH) content and agglomerate size on mechanical, compressional and drug release properties of agglomerates prepared by crystallo-co-- agglomeration (CCA). Studies on optimized batches of agglomerates (BXT1 and BXT2) prepared by CCA have showed adequate sphericity and strength required for efficient tabletting. Trend of strength reduction with a decrease in the size of agglomerates was noted for both batches, irrespective of drug loading. However, an increase in mean yield pressure (14.189 to 19.481) with an increase in size was observed for BXT2 having BXH-talc (1:15.7). Surprisingly, improvement in tensile strength was demonstrated by compacts prepared from BXT2, due to high BXH load, whereas BXT1, having a low amount of BXH (BXH-talc, 1:24), showed low tensile strength. Consequently, increased tensile strength was reflected in extended drug release from BXT2 compacts (Higuchi model, R 2 = 0.9506 to 0.9981). Thus, it can be concluded that interparticulate bridges formed by BXH and agglomerate size affect their mechanical, compressional and drug release properties.

The aim of the present study was to design a novel/conceptual delivery system using ibuprofen, anticipated for chronotherapy in arthritis with porous material to overcome the formulation limits (multiple steps, polymers, excipients) and to optimize drug loading for a desired release profile suitable for in vitro investigations. The objective of this delivery system lies in the availability of maximum drug amount for absorption in the wee hours as recommended. Drug loading using 3(2) factorial design on porous carrier, synthesized by high internal phase emulsion technique using styrene and divinylbenzene, was done via solvent evaporation using methanol and dichloromethane. The system was evaluated in vitro for drug loading, encapsulation efficiency, and surface characterization by scanning electron, atomic force microscopy, and customized drug release study. This study examined critical parameters such as solvent volume, drug amount, and solvent polarity on investigations related to drug adsorption and release mostly favoring low-polarity solvent dichloromethane. Overall release in all batches ranged 0.98-52% in acidic medium and 71-94% in basic medium. These results exhibit uniqueness in achieving the least drug release of 0.98%, an ideal one, without using any release modifiers, making it distinct from other approaches/technologies for time and controlled release and for chronotherapy.

The purpose of this study was to improve the entrapment efficiency of the water-soluble drug metronidazole using internal cross-linking agents. Calcium pectinate beads containing metronidazole were prepared by dropping a drug-pectin solution in 1% and 5% (m/V) calcium chloride for surface cross-linked beads. For the core cross-linked beads calcium carbonate was dispersed in the drug-pectin solution. The beads were characterized by particle size, swelling ratio, SEM, DSC, and in vitro drug release. It was found that the beads obtained by core cross-linking produced more drug entrapped beads than the surface cross-linked beads. Beads obtained using 1% (m/V) calcium chloride showed more drug entrapment than these obtained using 5% calcium chloride. The core cross-linking of pectin beads reduced drug loss by about 10-20%. The water lodging capacity of beads depended upon gel strength which is a function of the internal gelling agent and pectin concentration. Complete drug release was observed within 30-60 min in the acidic dissolution medium. This work has showed that the core cross-linking agent increases the water-soluble drug entrapment in calcium pectinate beads.

The purpose of this research was to develop a stable bladder instillation of EO-9 for the treatment of superficial bladder cancer. First, stability and dissolution studies were performed. Subsequently, the freeze-drying process was optimized by determination of the freeze-drying characteristics of the selected cosolvent/water system and differential scanning calorimetry analysis of the formulation solution. Furthermore, the influence of the freeze-drying process on crystallinity and morphology of the freeze-dried product was determined with x-ray diffraction analysis and scanning electron microscopy, respectively. Subsequently, a reconstitution solution was developed. This study revealed that tert-butyl alcohol (TBA) can be used to both dramatically improve the solubility and stability of EO-9 and to shorten the freeze-drying cycle by increasing the sublimation rate. During freeze drying, 3 TBA crystals were found: TBA hydrate-ice crystals, crystals of TBA hydrate, and a third crystal, probably composed of TBA hydrate crystals containing approximately 90% to 95% TBA. Furthermore, it was shown that crystallization of TBA hydrate was inhibited in the presence of both sodium bicarbonate (NaHCO3) and mannitol. Addition of an annealing step resulted in a minor increase in the crystallinity of the freeze-dried product and formation of the delta-polymorph of mannitol. A stable bladder instillation was obtained after reconstitution of the freeze-dried product (containing 8 mg of EO-9, 20 mg of NaHCO3, and 50 mg of mannitol per vial) to 20 mL with a reconstitution solution composed of propylene glycol/water for injection (WfI)/NaHCO3/sodium edetate 60%/40%/2%/0.02% vol/vol/wt/wt, followed by dilution with WfI to a final volume of 40 mL.

Summary Background Excessive transepidermal water loss (TEWL) is the one of the causes of dry skin, and skin moisturizers have been used to overcome it. Aim The purpose of this research was to study the moisturizing effect of sericin, a silk protein. Because silk sericin has resemblance with the natural moisturizing factor (NMF), it has been studied for its application in skin cosmetics. Methods Sericin gels were prepared using sericin solution and with pluronic and carbopol as stabilizers. The gels were applied on the skin of healthy human volunteers and its moisturizing efficiency was evaluated by measuring the skin hydroxyproline content, impedance, TEWL, and scanning electron microscopy (SEM) results. Results Decrease in skin impedance, increase in hydroxyproline level, and hydration of epidermal cells revealed the moisturizing effect of sericin, whereas decrease in the value of TEWL may be attributed to occlusive effect, which prevents water loss from the upper layer of the skin. Skin surface topography revealed the smoothness of the upper layer of the skin as a result of moisturization. Conclusion Increase in the intrinsic moisturization of skin by sericin may be attributed to restoration of the amino acids and its occlusive effect. Thus, it would become a promising and important moisturizing ingredient in moisturizing formulations.

The aim of the present study was to obtain cross-linked calcium-gellan beads containing diclofenac sodium as model drug, using full 3(3) factorial design. Drug quantity, pH of cross-linking solution, and speed of agitation were selected as variables for factorial design. The resultant beads were evaluated by scanning electron microscopy (SEM), percent yield, entrapment efficiency, micromeritic properties, swelling and drug release studies. The drug-loaded beads were spherical with size range of 0.85-1.8 mm. Percent yield and entrapment efficiency of various batches were in the range of 86.48-98.28% w/w and 72.52-92.74% w/w, respectively. Calcium-gellan beads containing diclofenac sodium showed pH-dependent swelling and drug release properties. Swelling and drug release were significantly higher in pH 7.4 phosphate buffer than 0.1N HCl. The swelling ratio for beads was up to 22 and 3 for phosphate buffer and 0.1N HCl, respectively. Cumulative diclofenac sodium release from calcium-gellan beads was 12-35% in 0.1N HCl within 2 h, whereas complete drug release was observed within 3-4 h in pH 7.4 phosphate buffer.

The purpose of this work was to develop hollow calcium pectinate beads for floating-pulsatile release of diclofenac sodium intended for chronopharmacotherapy. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. To overcome limitations of various approaches for imparting buoyancy, hollow/porous beads were prepared by simple process of acid-base reaction during ionotropic crosslinking. The floating beads obtained were porous (34% porosity), hollow with bulk density

The purpose of this research was to obtain directly compressible agglomerates of ibuprofen-paracetamol containing a desired ratio of drugs using a crystallo-co-agglomeration technique. Crystallo-co-agglomeration is an extension of the spherical crystallization technique, which enables simultaneous crystallization and agglomeration of 2 or more drugs or crystallization of a drug and its simultaneous agglomeration with another drug or excipient. Dichloromethane (DCM)-water system containing polyethylene glycol (PEG) 6000, polyvinyl pyrollidone, and ethylcellulose was used as the crystallization system. DCM acted as a good solvent for ibuprofen and bridging liquid for agglomeration. The process was performed at pH 5, considering the low solubility of ibuprofen and the stability of paracetamol. Loss of paracetamol was reduced by maintaining a low process temperature and by the addition of dextrose as a solubility suppressant. The agglomerates were characterized by differential scanning calorimetry, powder x-ray diffraction (PXRD), and scanning electron microscopy and were evaluated for tableting properties. The spherical agglomerates contained an ibuprofen-paracetamol ratio in the range of 1.23 to 1.36. Micromeritic, mechanical, and compressional properties of the agglomerates were affected by incorporated polymer. The PXRD data showed reduction in intensities owing to dilution and reduced crystallinity. Thermal data showed interaction between components at higher temperature. Ethylcellulose imparted mechanical strength to the agglomerates as well as compacts. The agglomerates containing PEG have better comparessibility but drug release in the initial stages was affected owing to asperity melting, yielding harder compacts. The agglomeration and properties of agglomerates were influenced by the nature of polymer.

Plumbagin, a bioactive natural lipophilic molecule, has wide pharmacological actions. It shows solubility limited low oral bioavailability. The aim of this study was to improve biopharmaceutical properties of plumbagin using crystal engineering techniques. Plumbagin crystals were prepared using anti-solvent precipitation (PPL), melt solidification (MPL), melt quenching (MQPL), sonocrystallization (SPL) and melt sonocrystallization (MSPL) processes and compared with properties of reference plumbagin. No significant changes in solubility and dissolution rate were observed for sintered MPL and MQPL crystals, whereas slightly higher Q 30min (cumulative percentage release in 30 min) and lower t 50% (time required for 50% w/w drug release) was observed for irregular shaped PPL crystals due to a two-fold decrease in the crystal size. As compared to needle shaped reference plumbagin crystals, the spongy and thread shaped crystals of SPL and MSPL showed two- and three-fold increase in solubility, seven- and eight-fold increase in Q 30min due to five- and ten-fold reduction in crystal size with increased surface area and reduced diffusion pathway of SPL and MSPL, respectively. Higher sonication amplitude, time, concentration and lower processing temperature favored formation of smaller crystals due to instantaneous supersaturation and nucleation. DSC and FT-IR spectra did not show significant difference. Low-intensity peaks in x-ray diffraction and improved flow properties were noticed for SPL and MSPL. Moreover, an in vivo study in Wistar rats also justified improvement in the therapeutic efficacy of SPL and MSPL. The study demonstrated the utility of sonoprocess to improve pharmaceutical properties of bioactive plumbagin.

Plumbagin recrystallised by cold crystallisation technique using a variety of polar and non-polar solvents was investigated for pharmaceutical properties. Different solvents gave varying sized and shaped plumbagin. Powder X-ray diffraction, differential scanning calorimetery and fourier transform infrared spectroscopy too confirmed differing crystal habit. Platy crystals, the most significant forms, obtained from cyclohexane possessed small size (62.93 ± 3.74 μm), higher bulk density (0.108 ± 0.014 g/ml) and lower enthalpy of fusion (∆H 62.62 ± 3.67 J/g). These demonstrated approximately two-fold increase in saturation solubility (155.01 ± 3.86 μg/ml), higher Q5min (cumulative percentage dissolution in 5 min) and lower t65% (time required for 65% dissolution) owing to greater surface area. In-vivo anti-inflammatory study in Wistar rats demonstrated improvement in therapeutic efficacy of recrystallised plumbagin. In conclusion surface modification led to enhanced efficacy of plumbagin; an approach capable of improving the bioavailability and clinical efficacy of other poorly water soluble phytomedicine.

Polymeric nanoparticles are advantageous in cancer therapy as they improve the physicochemical properties of drugs and consequently their behaviour in-vitro and the bioavailability of drugs. Andrographolide is a bioactive phytoconstituent widely used in the treatment of various tumours. However, the clinical efficacy by oral administration is contrasted by its biopharmaceutical properties. Hence an alternative dosage form and route of administration is investigated in the present study to enhance its therapeutic efficacy. Sustained release injectable andrographolide-loaded biodegradable poly(e-caprolactone) (PCL) nanoparticle suspension was prepared by a solvent displacement process using poly(ethylene oxide) -poly(propylene oxide)-poly(ethylene oxide) (PEO?PPO?PEO) triblock polymeric stabiliser (Pluronic® F-68/Pluronic® F-127). The nanoparticles were characterised in terms of particle size, encapsulation efficiency, zeta potential, surface morphology and crystallinity. In-vitro drug release studies were carried out in presence and absence of the enzyme Candida rugose lipase in phosphate-buffered saline (PBS, pH 7.4) at 37°C using the dialysis bag diffusion technique. The obtained suspended nanoparticles were spherical in shape with particle size of 226 ± 2 to 339 ± 5 nm and zeta potential −25.2 ± 1.6 to −27.7 ± 1.3 mV. Higher value of Q25hr (cumulative percentage release at the end of 25 h) and lower values of t50% and t80% (time required for 50% and 80% w/w drug release) indicated the suitability of PCL nanoparticles in controlled release, which followed diffusion mechanism. The study suggested the applicability of PCL nanoparticles to improve the biopharmaceutical properties of phytoconstituents in cancer chemotherapy.

The objective of this work was to develop matrix sustained-release tablets of highly water-soluble tramadol HCl using natural gums (xanthan [X gum] and guar [G gum]) as cost-effective, nontoxic, easily available, and suitable hydrophilic matrix systems compared with the extensively investigated hydrophilic matrices (ie, hydroxypropyl methylcellulose [HPMC]/carboxymethyl cellulose [CMC] with respect to in vitro drug release rate) and hydration rate of the polymers. Matrix tablets of tramadol (dose 100 mg) were produced by direct compression method. Different ratios of 100:0, 80:20, 60:40, 20:80, 0:100 of G gum (or X):HPMC, X gum:G gum, and triple mixture of these polymers (G gum, X gum, HPMC) were applied. After evaluation of physical characteristics of tablets, the dissolution test was performed in the phosphate buffer media (pH 7.4) up to 8 hours. Tablets with only X had the highest mean dissolution time (MDT), the least dissolution efficiency (DE(8)%), and released the drug following a zero-order model via swelling, diffusion, and erosion mechanisms. Guar gum alone could not efficiently control the drug release, while X and all combinations of natural gums with HPMC could retard tramadol HCl release. However, according to the similarity factor (f(2) ), pure HPMC and H(8)G(2) were the most similar formulations to Topalgic-LP as the reference standard.

The purpose of this research work was to obtain directly compressible agglomerates of ibuprofen with talc by a novel crystallo-co-agglomeration (CCA) technique, which is an extension of spherical crystallization. Ibuprofen-talc agglomerates were prepared using dichloromethane (DCM)-water as the crystallization system. DCM acted as a good solvent for ibuprofen as well as a bridging liquid for agglomeration of crystallized drug with talc. The agglomerates were characterized by differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy and were evaluated for tableting properties and for drug release. The process yielded spherical agglomerates containing ~95% to 96% wt/wt of ibuprofen. Agglomerates containing talc showed uniform distribution of hydroxypropylmethylcellulose and decreased crystallinity, and deformed under pressure. The miniscular form of ibuprofen and the hydrophobicity of talc governed the drug release rate. The batch containing a higher proportion of talc showed zero-order kinetics and drug release was extended up to 13 hours. The CCA technique developed in this study is suitable for obtaining agglomerates of drug with talc as an excipient.

The purpose of this research was to study the effect of concentration of polyethylene glycol and ethyl cellulose on the properties of agglomerates of ibuprofen-paracetamol obtained by crystallo-co-agglomeration technique. The process of crystallo-co-agglomeration involved recrystallization of ibuprofen and its simultaneous agglomeration with paracetamol in presence polymers. The effect of combination of polyethylene glycol and ethylcellulose was studied by 2 2 factorial design. Ibuprofen content of the agglomerate increased with increase in ethyl cellulose while paracetamol content was decreased with increase in polyethylene glycol. Differential scanning calorimetry thermograms of agglomerates showed the unchanged endotherm for ibuprofen melting, whereas paracetamol endotherm was diffused with low enthalpy. The agglomerates were spherical but increase in polyethylene glycol caused its deformation. Agglomerates containing ethylcellulose with polyethylene glycol have higher resistance for fragmentation, modulus of elasticity but impart high tensile strength.