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PubMed2006

The influence of PVP incorporation on moisture-induced surface crystallization of amorphous spray-dried lactose particles.

We have recently shown that atomic force microscopy (AFM) may be an appropriate method for characterisation of the re-crystallization of amorphous particles. In this study, spray-dried composite particles consisting of lactose and polyvinyl pyrrolidon (PVP) were characterised by AFM and electron spectroscopy for chemical analysis (ESCA), and their response on increasing the relative humidity (RH) was investigated. The PVP content in the particles used was 0, 5 or 25 wt.% of either PVP K17 or PVP K90. All composite particles were found to be enriched with PVP at the surface. The incorporation of PVP in the particles influenced the way the particles responded to an increase in RH. The specific RH interval in which the surface of the particles smoothened and the RH where crystallization could be detected, increased with an increase in the amount and molecular weight of the PVP in the particles. The crystallization kinetics of single particles was analysed with AFM and by utilising the JMAK equation. The rate constant for this transformation increased in an exponential manner with increasing RH. Furthermore, above the RH needed for the crystallization to occur, the exponential increase in the crystallization rate was larger for particles with higher polymer content which indicates that the stabilising effect decreases as the water content in the particles becomes higher. In this study we report a method for determination of crystallization kinetics on single composite particles, which is valuable when evaluating the effect of stabilisers in amorphous powders.

Crystallization↗
PubMed2003

Effect of spray-dried bovine serum on intake, health, and growth of broilers housed in different environments.

Three experiments utilizing broilers were conducted in different environments to evaluate the effects of Innavax (INX; spray-dried serum) administered in drinking water on broiler performance. In Exp. 1 (1 to 42 d), 252 Ross x Cobb male broilers were assigned randomly to one of six treatments consisting of tap water mixed with 0, 0.25, 0.50, 0.75, 1.0, or 1.25% (wt/wt) INX. Broilers (six broilers per pen; seven pens per treatment) were housed in Petersime battery cages (raised wire flooring) in temperature-controlled rooms. Average daily gain, and feed and water intake (as-fed) were not affected (P > 0.05) by experimental treatments. Feed efficiency tended to improve linearly (P = 0.076) from d 0 to 7 with increasing levels of INX, but was unaffected (P > 0.05) during the remaining periods. In Exp. 2 and 3, 800 Ross x Ross 308 male broilers (400 broilers in each trial; 10 broilers per pen; 10 pens per treatment) in two 21-d experiments were assigned randomly to one of four treatments consisting of tap water mixed with 0, 0.45, 0.90, or 1.35% (wt/wt) INX. Broilers were housed in floor pens containing clean (Exp. 2) or used (Exp. 3) litter. In Exp. 2, intake, ADG, and feed efficiency were linearly improved (P < 0.05) during the first week with increasing levels of INX. During the second week (d 8 to 14), ADG, water intake, and feed efficiency were linearly improved (P < 0.05) with increasing levels of INX. In the third week (d 15 to 21), ADG and feed and water intake were not affected (P > 0.10) by level of INX. Overall (d 0 to 21), ADG, intake, and feed efficiency were linearly improved (P < 0.05) with INX. In Exp. 3, ADG, water intake, and feed efficiency were linearly improved (P < 0.05) during each period. Feed intake was not affected (P > 0.05) by experimental treatment during d 0 to 7, but was linearly increased (P < 0.05) from d 8 to 14 and 15 to 21. The greatest growth response of broilers to INX was observed when broilers were housed in floor pens with used litter, followed by floor pens with clean litter and battery pens. Further research on the relationship between the response to INX and housing conditions seems warranted.

Animal Husbandry↗
PubMedDate not supplied

Preparation by spray drying of amphotericin B-phospholipid composite particles and their anticellular activity.

As a potent drug carrier for systemic fungal infections, amphotericin B(AmB)-phospholipid composite particles (APCPs) were prepared by the spray drying method. AmB and egg phosphatidylcholine, co-dissolved in methanol (0.0425-0.45 mg AmB/ml, 0.17-1.8 mg lipid/ml), was nebulized at 2 ml/min. The aerosol produced was carried by air at 1000 ml/min to the inner tubes of a serially connected distilling column system, of which the outer tubes were supplied with circulating water of 95 degrees C. The particles, by scanning electron microphotography, are spherical and submicronsized. Upon hydration of the particles in phosphate-buffered saline for 30 min at room temperature, liposome-like bilayer vesicles were formed along with AmB-phospholipid complexes, evidenced by the transmission electron microphotographs and the positive peak around 330 nm of the circular dichroism spectrum, respectively. The hemolytic abilities of the APCPs were lower than those of free drug, without loss of the antifungal activity. The suppressed hemolysis could be ascribed to the liposomes and to the complexes that are reconstituted by hydration of APCPs. The dry composite particles could circumvent the inherent instability of liposomal formulations.

Amphotericin B↗
PubMedDate not supplied

Quality improvement of spray-dried, protein-loaded D,L-PLA microspheres by appropriate polymer solvent selection.

The aim was to study the effect of the type of polymer solvent on characteristics of microspheres produced by spray drying. The water-soluble model protein, bovine serum albumin (BSA) was microencapsulated into biodegradable poly(D,L-lactic acid) using the following 10 different polymer solvents: acetaldehyde dimethyl acetal, acetone, dichloromethane, dioxane, ethyl acetate, ethyl vinyl ether, nitromethane, tetrahydrofuran, 1,1,1-trichloroethane, and 1,1,2-trichloroethylene. These solvents having similar toxicity levels differ greatly in their physico-chemical characteristics such as boiling point, vapour pressure, miscibility and interfacial tension with an aqueous phase, and solubility parameter. The effect of these solvents on microsphere morphology was studied by SEM-micrographs. Regular particle morphology was obtained when dichloromethane, ethyl acetate, or nitromethane was used as the polymer solvent, whereas the trichlorinated solvents, tetrahydrofuran, and dioxane produced a substantial number of coalesced particles. The results are interpreted in terms of boiling point, vapour pressure, and polymer-solvent affinity. Further, BSA-loading and -integrity in the microspheres, and burst release were analysed. The theoretical loading of 2.9% was attained with dichloromethane, ethyl acetate and nitromethane, in agreement with observations of particle morphology. HPLC- and SDS-PAGE analysis of the microencapsulated BSA did not show any protein degradation or dimerization, whereas solid-phase ELISA clearly revealed that the in vitro protein antigenicity was substantially reduced (50%), particularly by water miscible solvents. Dichloromethane and ethyl acetate did not show any detrimental effect on protein antigenicity. Finally, burst release could be related again to particle morphology, with dichloromethane and nitromethane giving a burst release of only 5%. In conclusion, dichloromethane, ethyl acetate and nitromethane proved to be the most suitable solvents for the polymer-protein system studied.

Animals↗
PubMed2002

The effect of alkylpolyglycoside surfactants on the crystallization of spray-dried salbutamol sulphate: a GravimetricNear-Infrared Spectroscopy Study.

This study monitored the effect of a series of structurally related surfactants on the crystallization of amorphous salbutamol sulphate. Amorphous salbutamol sulphate was prepared by spray drying from a solution in water and in the presence of various alkylpolyglycosides (APGs) at different concentrations. The particles were then analyzed using isothermal microcalorimetry and water vapor sorption (Dynamic Vapour Sorption, DVS) analysis combined with near-infrared spectroscopy (DVS-NIR). Both isothermal microcalorimetry and DVS-NIR were able to detect the transition from the amorphous to the crystalline state. The presence of APG surfactants modified the shape of the crystallization peak obtained using isothermal microcalorimetry. The gravimetric study combined with NIR revealed that while the crystallization was similar for the particles with or without surfactant, there was a great difference in the release of water from the newly formed crystal. In the presence of some of the surfactants tested, salbutamol sulphate released the water much faster than in the absence of surfactant. These results helped to explain the differences found in the isothermal microcalorimeter data. Differences were observed in the shapes of the NIR water peaks related to water due to the presence of the surfactant. In conclusion, the use of DVS combined with NIR has helped to analyze and understand the effect of APGs on the crystallization of amorphous salbutamol sulphate.

Albuterol↗
PubMedDate not supplied

Oxidation of linoleic acid encapsulated with gum arabic or maltodextrin by spray-drying.

Linoleic acid was emulsified with gum arabic or maltodextrin at various weight ratios of the acid to the polysaccharide in the presence or absence of a small-molecule emulsifier. The emulsions were spray-dried to produce microcapsules. Emulsions prepared with gum arabic were smaller in droplet size and more stable than those prepared with maltodextrin, and linoleic acid in a gum arabic-based microcapsule was also most resistant to oxidation than that in a maltodextrin-based microcapsule. Although the oil droplet size in the emulsion with maltodextrin decreased and the emulsion stability was improved by addition of a small-molecule emulsifier to linoleic acid, the oxidative stability of the encapsulated linoleic acid was not significantly improved. Encapsulated linoleic acid of small droplet size oxidized more slowly than that of large droplet size.

Drug Compounding↗
PubMed2002

Modifying the release of leuprolide from spray dried OED microparticles.

A range of oligosaccharide ester derivatives (OEDs) have been designed as drug delivery matrices for controlled release. The synthetic hormone analogue, leuprolide, was encapsulated within these matrices using hydrophobic ion pairing and solvent spray drying. The particles produced modified the release of leuprolide in vitro (dissolution in phosphate buffered saline) and in vivo (subcutaneous and pulmonary delivery in the rat). Release rate was dependent on drug loading and could be manipulated by choice of OED and by combining different OEDs in different ratios. Leuprolide encapsulated in the OEDs retained biological activity as evidenced by elevation in plasma luteinising hormone levels following subcutaneous injection of leuprolide recovered from OED particles in vitro prior to in vivo administration.

Administration, Inhalation↗
PubMed2002

Effect of spray-dried plasma and lipopolysaccharide exposure on weaned pigs: I. Effects on the immune axis of weaned pigs.

A study was conducted with 20 weaned barrows (14 d, 4.98 +/- .21 kg) to determine the effect of spray-dried plasma (SDP) on the pig's immune response to a lipopolysaccharide (LPS) challenge. After weaning, pigs were fed a diet containing 0 or 7% SDP for 7 d. On d 6 postweaning, all pigs were fitted with a jugular catheter. On d 7 postweaning, the pigs were given an i.p. injection of either saline or LPS (150 microg/kg BW) followed by a 3-h blood collection every 15 min. Following blood collection, all pigs were killed and tissue was collected for mRNA analysis. Additionally, the small intestine was collected for measurement of villus height, crypt depth, and villus height:crypt depth ratio (VCR) at three sites (25, 50, and 75% of the total length). Feeding SDP resulted in reduced (P < 0.05) mRNA expression of tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta) mRNA in the adrenal gland, spleen, hypothalamus, pituitary gland, and liver. Additionally, expression of IL-6 mRNA was reduced (P < 0.05) in the spleen and pituitary gland for pigs fed SDP. For pigs fed the diet with SDP, LPS administration did not affect (P > 0.10) cytokine mRNA expression, whereas LPS reduced expression of TNF-alpha mRNA in the spleen and IL-1beta mRNA in the adrenal gland, spleen, and thymus for pigs fed the diet without SDP. For pigs fed the diet with SDP, LPS caused serum TNF-alpha to increase 150-fold compared to a 60-fold increase for pigs fed the diet without SDP. Similarly, interferon-gamma (IFN-gamma) increased 110-fold for pigs fed the diet with SDP compared to a 16-fold increase for pigs fed the diet without SDP. For pigs fed the diet with SDP, LPS caused major villus atrophy, whereas for pigs fed the diet without SDP, LPS had no effect on intestinal morphology. These results demonstrate that the basal activation of the immune system appears to be less for pigs fed the diet with SDP compared to pigs fed the diet without SDP after weaning. Additionally, for pigs fed the diet with SDP, there appeared to be an overresponse of the immune system following LPS administration, which resulted in major damage to the mucosa of the gastrointestinal tract.

Adrenal Glands↗
PubMed2003

Response of early-weaned pigs to an enterotoxigenic Escherichia coli (K88) challenge when fed diets containing spray-dried porcine plasma or pea protein isolate plus egg yolk antibody.

Enterotoxigenic E. coli (ETEC) infection and resulting scours is a major problem for young pigs, especially when purified plant proteins are fed rather than spray-dried porcine plasma (SDPP). The effect of supplementing a pea protein isolate (PPI)-based diet with egg yolk antibodies (EYA) from laying hens immunized with ETEC K88 antigen on piglet performance, incidence of scours, and gut histology was studied in a 14-d trial. Ninety-six 10-d-old weaned pigs were assigned to five dietary treatments in a completely randomized design to give six replicate pens per treatment. The treatments were PPI without EYA (PPI-EYA), PPI with EYA (PPI+EYA), SDPP without EYA (SDPP-EYA), SDPP with EYA (SDPP+EYA), or a combination of PPI and SDPP (PPI+SDPP). Diets were formulated to similar nutrient levels and provided for ad libitum intake. Blood from all pigs was taken on d 0, 7, and 14 for determining plasma urea N (PUN). On d 7, pigs were orally challenged with 6 mL of 10(10) cfu/ mL ETEC K88. Piglets were weighed on d 7 and 14. On d 7, 8, and 14, four pigs per treatment were sacrificed to study the histology of the small intestine. Weekly feed intake, BW changes, and gain:feed were determined. Fecal swabs from 10 pigs per treatment were taken for a PCR test to detect K88 E. coli. Feed efficiency over the 14-d period was not affected (P > 0.78) by dietary treatment. Mean ADFI on an as-fed basis was lower (P < 0.002) in piglets fed PPI-EYA (64.3 g/d) compared with PPI+EYA (94.8 g/d) or SDPP (102 g/d) during wk 1. Piglets fed PPI-EYA tend to have a lower (P < 0.026) overall ADG (84 g/d) than those fed PPI+EYA (123 g/d) or SDPP (127 g/d) (P < 0.006)-based diets. Although scours was evident in all groups of pigs 6 h after the challenge, most of the piglets fed EYA- or SDPP-containing diets recovered 10 to 72 h postchallenge, whereas those fed PPI-EYA continued to have severe diarrhea, resulting in 33% mortality. The PCR results showed that a greater (P < 0.01) percentage of piglets fed PPI-EYA compared with those fed SDPP- or EYA-containing diets continued to shed ETEC K88 at the end of the 14-d study. Piglets fed PPI-EYA had shorter villi (P < 0.01), higher intestinal pH (P < 0.013), and higher PUN (P < 0.05) than those fed the SDPP- or EYA-containing diets during the entire 14-d study. It was concluded that specific EYA and SDPP could provide passive control of ETEC infection and potentially improve feed intake and weight gain in young pigs fed PPI.

Animal Feed↗
PubMed1994

Effect of spray-dried porcine plasma protein on feed intake, growth rate, and efficiency of gain in mice.

One hundred eight mice were weaned at 21 +/- 1 d and allotted to four dietary treatments: 1) control, 2) control + 4% spray-dried porcine plasma protein (SDPP), 3) control + 8% SDPP, and 4) control + 12% SDPP. Daily gain for males increased with increasing SDPP during wk 1 (P < .01), wk 2 (P < .01), and for the entire 3 wk (P < .01). Daily gain increased quadratically with increasing SDPP for females during wk 1 (P < .05). During the 3rd wk, ADG decreased for females with increasing SDPP (P < .05). Daily feed intake increased linearly (P < .01) with increasing SDPP in all periods. Gain-to-feed ratio (G/F) increased with increasing SDPP during wk 1 (P < .01) and for the first 2 wk (P < .05). During wk 3, G/F decreased with increasing SDPP level (P < .01). Gain-to-feed ratio of females responded quadratically to increasing SDPP during wk 1 (P < .05), whereas G/F of males increased linearly with increasing SDPP level. Gain-to-feed ratio for the entire trial was unaffected by treatment among females (P = .82) but increased linearly with increasing SDPP levels among males (P < .01). Liver weight increased quadratically with increasing SDPP levels for males (P < .05) and females (P < .05). Treatment effect on liver weight per kilogram BW.75 approached significance (P < .10) in females. Male liver weight/100 g BW and liver weight per kilogram BW.75 responded quadratically to increasing SDPP levels (P < .05).(ABSTRACT TRUNCATED AT 250 WORDS)

Aerosols↗
PubMed2000

Effects of a whey protein product and spray-dried animal plasma on growth performance of weanling pigs.

Five experiments were conducted to evaluate the effects of a high-protein, whey protein product (WPP; 73% CP, 6.8% lysine, 12.8% fat, and 5% lactose) and spray-dried animal plasma (SDAP) on growth performance of weanling pigs. In all experiments, pigs were fed experimental diets from d 0 to 14 after weaning in a pelleted form and then a common diet in meal form for the remainder of the experiment. Dietary treatments were established by substituting WPP or SDAP for dried skim milk (Exp. 1) or soybean meal (Exp. 2, 3, 4, and 5) in the control diet. In Exp. 1, we maintained a constant level of lactose in all diets by adjusting the amount of added crystalline lactose. The amount of lactose in diets used in Exp. 2 through 5 varied slightly by the addition of WPP. In Exp. 1 and 2, 180 weanling pigs (initially 5.8 kg and 19 +/- 1 d of age or 5.5 kg and 17 +/- 1 d of age, respectively) were used. Treatment diets contained SDAP (2.5 and 5%) or WPP (2.7 and 5.4% in Exp.1, and 2.5 or 5.0% in Exp. 2). In Exp. 1, from d 0 to 7 after weaning, ADG and ADFI increased with increasing SDAP (linear, P < .01). No other treatment effects were observed during the d 0 to 14 period. In Exp. 2, from d 0 to 14 after weaning, ADG and G:F increased (linear, P < .04) with increasing SDAP or WWP. In Exp. 3, 305 weanling pigs (initially 4.1 kg and 12 +/- 1 d of age) were used. The control diet contained 2.5% SDAP. The experimental diets were similar to the control diet but contained an additional 2.5 or 5.0% SDAP or 2.5 or 5.0% WPP. From d 0 to 14 after weaning, ADG, ADFI, and G:F increased (quadratic, P < .05) with increasing SDAP up to 5.0%. Increasing WPP increased ADG (quadratic, P < .07) and ADFI (linear, P < .09). In Exp. 4 and 5, 329 and 756 weanling pigs (initially 4.1 kg and 12 +/- 1 d of age and 5.2 kg and 18 +/- 1 d of age, respectively) were fed diets in which WPP was substituted for 0, 25, 50, 75, and 100% (Exp. 4) or 0, 50, and 100% (Exp. 5) of the SDAP in the control diet. In Exp. 4 and 5, from d 0 to 14 after weaning, pigs fed a 1:1 blend of each protein source had better ADG (quadratic, P < .04) than those only fed SDAP. In conclusion, WPP can be used in combination with or as a total replacement for SDAP in diets for weanling pigs without reducing performance.

Animal Feed↗
PubMed2006

Growth response of broilers to spray-dried plasma in pelleted or expanded feed processed at high temperature.

A series of 4 experiments evaluated effects of mash conditioning temperature from a pellet mill or expander on performance of broilers fed pelleted diets containing spray-dried plasma (SDP). All experiments utilized Ross x Ross 308 male broilers randomly assigned to their respective treatments (6 or 10 broilers/pen and 8 or 10 pens/treatment). Treatments in Exp. 1 consisted of a control (0% SDP), SDP coated postpelleting, or SDP blended into the meal prepelleting. Experiment 2 and 3 included the same 3 treatments as in Exp. 1 but with additional treatments of SDP blended into the meal and conditioned at 90 or 95 degrees C before pelleting. In Exp. 4, treatments consisted of a control (0% SDP) or SDP blended into the meal and pelleted (85 degrees C conditioning temperature) or expanded (149 degrees C final effective temperature) and then pelleted. Corn-soybean meal-based diets were formulated to be equal in lysine and ME in all experiments. Pelleted diets were conditioned for 15 s at 85 degrees C, and expanded diets were conditioned at 95 degrees C, 29.7 MJ/t, 13.95 kg/cm2 cone pressure, exit temperature of 149 degrees C, and then pelleted through a 4 x 32-mm die. In Exp. 1, ADG and feed intake were improved (P < 0.05) for broilers fed SDP from d 1 to 28 of age, with greater BW at d 42. In Exp. 2, both in early (d 1 to 28 of age) phases, and overall (d 1 to 42 of age), broilers fed SDP had improved (P < 0.05) gain and efficiency. In Exp. 3, ADG, feed intake, efficiency of gain, and BW were improved (P < 0.01) for broilers fed SDP from d 1 to 21 of age, regardless of conditioning temperature. In Exp. 4, broilers fed SDP had improved (P < 0.05) gain, BW, and feed intake regardless of processing method. Overall, the results of all of the experiments demonstrated that pellet conditioning temperature from 85 to 95 degrees C and expander temperatures to 149 degrees C did not impair the positive growth effects of SDP in pelleted or expanded broiler feed.

Animal Feed↗
PubMed1994

Piroxicam release from spray-dried biodegradable microspheres.

Poly(D,L-lactide) (DL-PLA) and poly(D,L-lactide-co-glycolide) (DL-PLGA) microspheres containing a non-steroidal anti-inflammatory model drug, piroxicam, were prepared by a spray drying process. The microspheres were characterized for surface morphology by scanning electron microscopy, particle size distribution by laser diffraction spectrometry, drug content and in vitro drug release. The diameters of the microspheres ranged from 1 to 15 microns. The DL-PLA particles appeared to be more spherical and smooth than the DL-PLGA particles, which showed a more undulated surface. Piroxicam content in the microspheres was 10%. A very high encapsulation efficiency of 99.0% was achieved with both polymers. In vitro release studies were carried out in a flow-through cell. The in vitro release rate of the drug from the DL-PLA microspheres was very slow. Less than 20% of the loaded drug was released within 10 d. The release mechanism was diffusion controlled and followed a square root of time relationship. Only a very small initial burst effect was observed. In contrast, the DL-PLGA microspheres provided a much faster drug release: about 50% was released within the first 5 h of the experiment. The mechanism for piroxicam release from the DL-PLA microspheres is not matrix erosion, but mainly drug diffusion through the intact polymer barrier. For the DL-PLGA microspheres, a pore diffusion release mechanism is proposed.

Biodegradation, Environmental↗
PubMed2001

Improved dissolution and cytotoxicity of camptothecin incorporated into oxidized-cellulose microspheres prepared by spray drying.

Oxidized celluloses (OC) containing 7, 13, and 20% carboxylic content (OC-7, OC-13, and OC-20, respectively) have been converted into aqueous colloidal dispersions and used to prepare microspheres of the antineoplastic agent camptothecin (CPT) by spray drying. Plasticizers used were glycerin, polyethylene glycol 400 (PEG-400), and polyethylene glycol 6000 (PEG-6000). Irrespective of the carboxyiic content of OC and the nature of plasticizer employed, the size of microspheres varied from 1.25+/-0.40 to 1.52+/-0.47 microm. The release studies in pH 7.4 buffer revealed the dissolution of CPT to be faster from the microsphere formulations than from physical mixtures and free CPT. The times to release 50% CPT (T-50%) from microspheres prepared using OC-7, OC-13, and OC-20 were about 31, 37, and 19 h, respectively. The in vitro cytotoxicity results indicated OC-20/CPT microspheres to be more effective than free CPT against human-derived RPMI-8402 lymphoid and THP-1 myeloid leukemia cell lines. The ED50 values for the OC-20/CPT microspheres and free CPT were 1 x 10(-5) and 0.25 x 10(-1) microg/mL, respectively, against the RPMI-8402 line and 0.5 x 10(-2) and 0.75 microg/mL, respectively, against the THP-1 line. The higher activity of OC-20/CPT microspheres compared to that of the free drug is attributed to increased dissolution of CPT from microspheres.

Antineoplastic Agents, Phytogenic↗
PubMed1998

Water vapor sorption studies on the physical stability of a series of spray-dried protein/sugar powders for inhalation.

One theory suggests that by maintaining the protein in an amorphous glassy sugar matrix, the physical hindrance encountered by the protein functions to stabilize it. Thus, the nature of the sugar/protein interaction is important as is the maintenance of the sugar in an amorphous form without any recrystallization. Moisture is known to function as a plasticizer and facilitate crystallization and thus loss of the amorphous state. We report the effect of cospray-drying with different proteins on the physical stability of lactose and mannitol. Particle sizing showed their suitability for inhalation, and the effect of exposure of the spray-dried products to moisture vapor was monitored gravimetrically. Bovine liver catalase, bovine pancreatic insulin, and bovine pancreatic ribonuclease A when individually cospray-dried with lactose showed no extensive initial crystallinity by powder X-ray diffraction, but proteins cospray-dried with mannitol generally showed evidence of mannitol component crystallinity. Catalase appeared to inhibit lactose crystallization from an amorphous matrix to a greater extent than insulin when exposed to short-term elevated humidity, but this difference was a kinetic feature. The hygroscopicities of the cospray-dried materials differed and indicated that each protein/sugar system required individual characterization to identify an optimal formulation.

Catalase↗
PubMed2004

Characterization of curcumin-PVP solid dispersion obtained by spray drying.

Curcumin, a naturally occurring highly lipophilic molecule has wide range of pharmacological activities. However, its limited aqueous solubility and degradation at alkaline pH restricts its bioavailability. Solid dispersions of curcumin in different ratios with PVP were prepared by spray drying. Physical characterization by SEM, IR, DSC, and XRPD studies, in comparison with corresponding physical mixtures revealed the changes in solid state during the formation of dispersion and justified the formation of high-energy amorphous phase. Dissolution studies of curcumin and its physical mixtures in 0.1 N HCl showed negligible release even after 90 min. Whereas, solid dispersions showed complete dissolution within 30 min. This may aid in improving bioavailability and dose reduction of the drug.

Calorimetry, Differential Scanning↗
PubMed2005

Novel powder formulations for controlled delivery of poorly soluble anticancer drug: application and investigation of TPGS and PEG in spray-dried particulate system.

Biodegradable poly (lactic-co-glycolic acid) (PLGA), D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) and/or polyethylene glycol (PEG) were combined as pharmaceutical excipient to fabricate microparticles containing sparingly soluble drug paclitaxel by spray-drying technique with successful achievement. The effect of formulation variety on particle morphology, surface composition, thermal property, drug entrapped capability, and drug release profile was investigated. The result indicated that the use of the appropriate mixtures of PLGA, TPGS and/or PEG produced paclitaxel-loaded microparticles characterised by acceptable pharmaceutical properties. Atomic force microcopy (AFM) and scanning electron microscopy (SEM) showed that the produced microparticles were spherical in shape with dimples or pores. The particle size ranged from 0.88 to 2.44 microm with narrow distribution. The combination of TPGS and PEG in the formulation resulted in a narrow particle size distribution in general although the influence of the formulation on the particle size was not significant. Differential scanning calorimetry (DSC) study implied that all those components in consideration were compatible well in the blend formulation systems. The paclitaxel entrapped in the particles existed in an amorphous or disordered-crystalline status in the matrices and was independent of the PLGA/TPGS/PEG ratio. X-ray photoelectron spectroscope (XPS) analysis revealed that after incorporation the particle's surface was dominated with PLGA due to its hydrophobic property. The formulation variety had an important impact on the drug release that was reduced with the presence of large fraction of TPGS resulting from a strong hydrophobic interaction between various matrix materials and the drug inside the particle. A zero order release could be yielded by optimising the ratio of PLGA/TPGS/PEG. The combination of PLGA/TPGS/PEG as safe pharmaceutical excipient to formulate particulate delivery system is beneficial in improving the pharmaceutical properties for further powder dosage application.

Antineoplastic Agents↗
PubMed2002

Suppressive effect of saturated acyl L-ascorbate on the oxidation of linoleic acid encapsulated with maltodextrin or gum arabic by spray-drying.

6-O-Palmitoyl L-ascorbate was added to linoleic acid at various molar ratios of the ascorbate to the acid, the mixtures were emulsified with a maltodextrin or gum arabic solution, and the emulsions were spray-dried to produce microcapsules. At higher molar ratios, the oil droplets in the emulsions were smaller, and the oxidative stabilities of the encapsulated linoleic acid were higher for both the maltodextrin- and gum arabic-based microcapsules. 6-O-Capryloyl, caproyl, and lauroyl L-ascorbates, which were synthesized through lipase-catalyzed condensation in acetone, were also used for the microencapsulation of linoleic acid. Except for capryloyl L-ascorbate, the addition of a saturated acyl ascorbate, especially caproyl ascorbate, to linoleic acid was effective for preparing oil droplets of small particle diameter and for suppressing the oxidation of the encapsulated linoleic acid.

Acylation↗