Scintigraphic Studies Research Articles

Optimization of nanostructured lipid carriers of lamotrigine for brain delivery: in vitro characterization and in vivo efficacy in epilepsy

Objective: The aim of the present work was to investigate the efficacy of nanostructured lipid carriers (NLCs) to enhance the brain targeting of lamotrigine (LMT) following intranasal (IN) administration.Methods: Formulation was optimized using four-factor three levels Box– Behnken design to establish the functional relationships between variables on responses, that is, particle size, entrapment efficiency (EE) and percentage cumulative drug release of LMT-loaded NLCs. NLCs were evaluated for particle size, surface morphology, %EE and in vitro release and ex vivo permeation. The developed formulation was subjected to stability study, in vivo efficacy and scintigraphic study in Wistar rat model.Results: The NLCs had a mean particle size of 151.6 ± 7.6 nm, polydispersity index of 0.249 ± 0.035, zeta potential of 11.75 ± 2.96 mV and EE of 96.64 ± 4.27%. The drug release from NLCs followed Fickian diffusion with a flux value of 11.73 μgcm−2h−1. Sustained drug concentration was obtained in NLCs carrying LMT after IN administration after 24 h. γ scintigraphy studies further proved high accumulation of drug in brain.Conclusion: Hence we can conclude that IN administration of LMT NLCs in rats is able to maintain higher brain concentration of LMT compared to IN and oral drug solution.

Preparation, Biodistribution, and Scintigraphic Evaluation of 99mTc-Clindamycin: an Infection Imaging Agent

Bacterial infection is found to be the cause of death throughout the world. Nuclear medicine imaging with the help of radiopharmaceuticals has great potential for treating infections. In the present work, clindamycin, a lincosamide antibiotic, was labeled with technetium-99m (~380MBq). Clindamycin has been proven to be efficient for treating serious infections caused by bacteria such as Staphylococcus aureus. Quality control, characterization, biodistribution, and scintigraphy of radiolabeled clindamycin were done, and labeling efficiency was determined by ascending paper chromatography. More than 95% labeling efficiency with technetium-99m ((99m)Tc) was achieved at pH6-7 while using 2.5-3μg SnCl2 · H2O as a reducing agent and 100μg of ligand at room temperature. The characterization of the compound was performed by using electrophoresis, HPLC and shake flask assay. Electrophoresis indicates the neutral behavior of (99m)Tc-clindamycin. HPLC analysis confirms the single specie of the labeled compound, while shake flask assay confirms high lipophilicity. The biodistribution studies of (99m)Tc-clindamycin were performed Sprague Dawley rats bearing bacterial infection. Scintigraphy and biodistribution studies showed a high uptake of (99m)Tc-clindamycin in the liver, heart, lung, and stomach as well as at S. aureus-infected sites in rabbits.

Statin therapy and cardiac sympathetic activity in patients with heart failure: A 123Iodine-metaiodobenzylguanidine myocardial scintigraphy study

Statin therapy and cardiac sympathetic activity in patients with heart failure: A 123Iodine-metaiodobenzylguanidine myocardial scintigraphy study

Diagnostic sensitivity of bone scintigraphy for equine stifle disorders.

Disorders of the stifle are a common cause of lameness in horses yet the accuracy of scintigraphy for diagnosis of stifle conditions is controversial. The aim of retrospective cross-sectional study was to determine the diagnostic sensitivity (Se) of bone scintigraphy in detecting stifle disease and to determine if two orthogonal scintigraphic images improve diagnostic Se. Horses that underwent scintigraphic examination during a two-year period were included. Horses were divided into two groups: group 1 (N = 23) had lameness that was localized to the stifle by intra-articular analgesia and group 2 (N = 182) had lameness that was localized to a different location. Scintigraphic studies (one image or two images) were independently and retrospectively analyzed by two radiologists (R1 and R2). Sensitivity, specificity (Sp) and predictive values (PV), and were calculated for each type of study (one image or two images) and for each radiologist (R1 or R2). The Se to detect stifle disorders varied between radiologists (29.2% and 20.8%). The Sp was 84.5% and 88.3%. When two images were evaluated a decrease in the positive PV for both readers occurred. The Cohen kappa coefficient (κ) between readers was poor when one image (0.084) or two images (0.117) were evaluated. Findings from this study indicated that bone-phase nuclear scintigraphy is reasonably specific but highly insensitive for detecting lameness originating from the stifle in a diverse population of both normal and affected horses. The addition of a caudal scintigraphic image acquisition did not improve diagnostic sensitivity.

Classification schema of symptomatic enterogastric reflux utilizing sincalide augmentation on hepatobiliary scintigraphy.

Enterogastric reflux (EGR) is the reflux of duodenal contents into the stomach. Hepatobiliary scintigraphy provides physiologic assessment of the biliary system and was used to test the hypothesis that presence and timing of EGR may be associated with infusion of sincalide, a surrogate of endogenous cholecystokinin. One hundred fifty-seven hepatobiliary scintigraphy studies were retrospectively reviewed. Data included EGR incidence on initial reports, incidence after masked second reads, and time of EGR onset in relation to sincalide infusion. EGR cases were then classified according to onset on pre-, post-, or both presincalide and postsincalide imaging. Time of EGR onset at 19-24 minutes after start of a 15-min sincalide infusion differed significantly from normal (p<0.0001). EGR was initially reported in 14 of 157 cases (8.9%) but found in 38 of 157 cases on masked second reads (24.2%), corresponding to a 15.3% discrepancy rate. The temporal association of EGR onset with sincalide infusion may identify patients with EGR mimicking chronic cholecystitis or biliary dyskinesia. A novel classification schema was therefore developed as a framework for future research, utilizing EGR onset in relation to pre-, post-, or both presincalide and postsincalide imaging as a hypothetical biomarker of clinically significant EGR.

Validation of IAEA software package for the analysis of scintigraphic renal dynamic studies: parameters of renal transit in children with renal pelvic dilatation.

The objectives of the study were to use the International Atomic Energy Agency (IAEA) software package for the analysis of scintigraphic renal dynamic studies to obtain values of curve parameters and excretory parameters in children with hydronephrosis and to validate the reliability of these numerical outputs by comparing with values established by consensus reports. Fifty children with hydronephrosis (median age, 16 months; 30 boys, 20 girls; 99 kidneys) underwent Tc-MAG3 diuresis renography. Studies were analyzed by 2 observers, and according to the assessment of images, renograms, and differential function, kidneys were classified as normal (42, kidneys contralateral to hydronephrotic kidney), hypotonic unobstructed (49), and obstructed (8). The IAEA software was applied to each renogram. The parameters analyzed were as follows: normalized residual activity at 20 minutes (NORA 20) and on postmicturition (PM) acquisition, output efficiency at 20 minute (OE 20), PM to maximum renal count ratio (PM/max), and mean transit time (MTT). Mean values for normal, hypotonic unobstructed, and obstructed kidneys were as follows: NORA 20: 0.25, 0.57, and 2.16; OE 20 (%): 94.5, 87, and 57; normalized residual activity on PM acquisition: 0.02, 0.03, and 0.27; PM/max: 0.01, 0.02, and 0.13; and MTT (minutes): 1.9, 3.5, and 8.9, respectively. Difference between obstruction/dilatation and normal/dilatation was significant (P < 0.0001), as well as the correlation between NORA 20/OE 20 (R = -0.982). Cutoff values to predict obstruction were as follows: NORA 20, 1.6; OE 20, 73%; NORA PM, 0.11; PM/max, 0.06; and MTT, 8.23 minutes. The IAEA software package gives reliable values of numerical parameters of renal excretion. The use of the software improves diagnostic accuracy of diuresis renography in children.

Heart involvement in systemic sclerosis: a combined echocardiographic and scintigraphic study.

The aim of this study is to investigate systemic sclerosis (SSc) patients without clinically evident heart disease for cardiac abnormalities. SSc patients and age- and sex-matched healthy controls from the hospital staff underwent transthoracic echocardiography for the assessment of the left ventricle (LV) morphology and function and estimation of the pulmonary artery systolic pressure (PASP). Patients further underwent stress-rest myocardial perfusion imaging (MPI) scintigraphy by single-photon emission computed tomography (SPECT). Thirty-seven patients were included (33 women, 19 with diffuse, and 18 with limited SSc). LV hypertrophy was more common in SSc patients than controls (24.3 vs 0%, p = 0.001). Impaired LV relaxation was found in 45.9% of patients and 40.5% controls (p = 0.639). Excluding patients with arterial hypertension, LV hypertrophy was still found in 23.1% and LV relaxation impairment in 38.5%. PASP over 30mmHg was found in 13 patients (35.1%), 11 of whom had no history of pulmonary arterial hypertension (PAH). Of 35 patients who underwent SPECT, 21 patients (60%) exhibited reversible LV perfusion defects. Their mean age was 51.8years; four patients were younger than 40years old and eight patients younger than 50years. In all cases, ischemia was graded as mild or moderate and in a single case, graded as significant. Subclinical heart involvement is common in SSc patients even in the younger age groups. LV hypertrophy and impaired relaxation, raised PASP, and ischemia on MPI with SPECT are found in a significant proportion of SSc patients. Careful screening of SSc patients for potential heart involvement and consultation by a cardiologist may be of value.

Relationship of Gastrointestinal Symptoms and Psychosocial Distress to Gastric Retention in Children

To determine whether gastrointestinal (GI) symptoms (abdominal pain, nonpain GI symptoms, nausea) and/or psychosocial distress differ between children with/without gastroparesis and whether the severity of GI symptoms and/or psychosocial distress is related to the degree of gastroparesis. Children aged 7-18 years (N = 100; 63 female patients) undergoing a 4-hour gastric emptying scintigraphy study completed questionnaires evaluating GI symptoms, anxiety, and somatization for this prospective study. Spearman correlation, Mann-Whitney, t-test, and χ(2) tests were used as appropriate for statistical analysis. Children with gastroparesis (n = 25) were younger than those with normal emptying (12.6 ± 3.5 vs 14.3 ± 2.6 years, P = .01). Because questionnaire responses from 7- to 10-year-old children were inconsistent, only patient-reported symptoms from 11- to 18-year-olds were used. Within this older group (n = 83), children with gastroparesis (n = 17) did not differ from children with normal emptying in severity of GI symptoms or psychosocial distress. In children with gastroparesis, gastric retention at 4 hours was related inversely to vomiting (r = -0.506, P = .038), nausea (r = -0.536, P = .019), difficulty finishing a meal (r = -0.582, P = .014), and Children's Somatization Inventory score (r = -0.544, P = .024) and positively correlated with frequency of waking from sleep with symptoms (r = 0.551, P = .022). The severity of GI symptoms and psychosocial distress do not differ between children with/without gastroparesis who are undergoing gastric emptying scintigraphy. In those with gastroparesis, gastric retention appears to be inversely related to dyspeptic symptoms and somatization and positively related to waking from sleep with symptoms.

Sinking-Magnetic Microparticles Prepared by the Electrospray Method for Enhanced Gastric Antimicrobial Delivery

A targeted oral drug delivery system is useful to improve the treatment of gastrointestinal diseases. A high density sinking dosage form can sink to the bottom of the stomach near the pylori sections to enhance gastric retention. However, it is difficult to achieve a high density sinking system using the traditional technology. In the current study, novel stomach-specific sinking magnetic microparticles (SMMPs) were prepared via the monoaxial electrospray method for enhanced gastric antimicrobial delivery. The size of SMMPs was approximately 5 μm, and the Fe3O4 nanoparticles were observed in the SMMPs by transmission electron microscopy (TEM). The density of SMMPs increased as the concentration of Fe3O4 nanoparticles in the electrospray inlet flow increased, with the maximum true density of approximately 3.52 g/cm(3). The SMMPs displayed strong magnetism in vitro and in vivo. They can settle down in water within 120 s in vitro, and the settling time decreased to 20 s under a magnetic field. Furthermore, an in vivo γ scintigraphy study demonstrated that (131)I labeled SMMPs were retained in the stomach for over 8 h, and an external permanent magnet can increase their gastric retention time even further. Using Helicobacter pylori as a model bacterium, amoxicillin-loaded SMMPs exhibited a significantly greater eradication of H. pylori compared to the free drug, in vivo. Our results suggested that electrospray is an effective technique to prepare the high density gastroretentive dosage forms. We have shown that stomach-specific SMMPs can supply better treatment for H. pylori infections and have the potential to be used in clinical practice.

Statin therapy decreases cardiac sympathetic activity in patients with left ventricular dysfunction: a 123l‐MIBG myocardial scintigraphy study (1169.9)

Convincing animal and human studies indicate that statin therapy decreases renal and muscle sympathetic nerve activity. Reduced cardiac sympathetic drive and innervation have also been reported as pleiotropic consequences of statin therapy in a rat coronary ligation model. This study then investigated whether these results could be translated to a clinical setting of human left ventricular dysfunction. Washout rate (WR) and heart‐to‐mediastinum (H/M) ratio, indexes of cardiac sympathetic activity and innervation density, were obtained from planar 123l‐metaiodobenzylguanidine myocardial scintigraphy images of patients undergoing long‐term statin [30±7 mg/day for at least a month] (7 men and 4 women, NYHA class II‐III, ejection fraction of 45±5%, age of 53±4, and body mass of 83±5 kg) and only standard drug therapy (7 men and 6 women, NYHA class II‐III, ejection fraction of 37±7%, age of 57±2 years, and body mass of 77±7 kg). Resting cardiovascular variables and lipid profiles were similar between groups. Statin users presented lower WR (Statin 29±2% vs. SDT 39±1, P&lt;0.05) whereas early (1.7±0.2 vs. 1.6±0.2, P&gt;0.05) and late (Statin 1.6±0.2 vs. SDT 1.6±0.4, P&gt;0.05) H/M were similar for both groups. Our findings partially extend the results of animal studies and indicate that statin therapy reduces cardiac sympathetic activity in patients with left ventricular dysfunction without changing innervation density.Grant Funding Source: Supported by CAPES, CNPq, FAPERJ, FINEP.

Nasal Deposition of Ciclesonide Nasal Aerosol and Mometasone Aqueous Nasal Spray in Allergic Rhinitis Patients

Sensory attributes of intranasal corticosteroids, such as rundown to the back of the throat, may influence patient treatment preferences. This study compares the nasal deposition and nasal retention of a radiolabeled solution of ciclesonide nasal aerosol (CIC-hydrofluoroalkane [HFA]) with a radiolabeled suspension of mometasone furoate monohydrate aqueous nasal spray (MFNS) in subjects with either perennial allergic rhinitis (AR) or seasonal AR. In this open-label, single-dose, randomized, crossover scintigraphy study, 14 subjects with symptomatic AR received a single dose of radiolabeled 74-μg CIC-HFA (37 μg/spray, 1 spray/each nostril) via a nasal metered-dose inhaler or a single dose of radiolabeled 200-μg MFNS (50 μg/spray, 2 sprays/each nostril), with a minimum 5-day washout period between treatments. Initial deposition (2 minutes postdose) of radiolabeled CIC-HFA and MFNS in the nasal cavity, nasopharynx, and on nasal wipes, and retention of radioactivity in the nasal cavity and nasal run-out on nasal wipes at 2, 4, 6, 8, and 10 minutes postdose were quantified with scintigraphy. At 2 and 10 minutes postdose, deposition of radiolabeled CIC-HFA was significantly higher in the nasal cavity versus radiolabeled MFNS (99.42% versus 86.50% at 2 minutes, p = 0.0046; and 81.10% versus 54.31% at 10 minutes, p < 0.0001, respectively; p values unadjusted for multiplicity). Deposition of radioactivity on nasal wipes was significantly higher with MFNS versus CIC-HFA at all five time points, and posterior losses of radiolabeled formulation were significantly higher with MFNS at 6, 8, and 10 minutes postdose. In this scintigraphic study, significantly higher nasal deposition and retention of radiolabeled aerosol CIC-HFA were observed versus radiolabeled aqueous MFNS in subjects with AR.

Preparation and evaluation of three mucoadhesive dosage forms using 99mTc–Ofloxacin

Preparation of three mucoadhesive formulations was optimized and pharmaceutically evaluated. Ofloxacin was radiolabeled with 99mTc and radiolabeled complex was characterized by HPLC. 99mTc–Ofloxacin was added as a tracer to the formulations namely Oflox C934, Oflox C940 and Oflox HPMC and the formulations were fed orally to rats. Imaging studies were carried out to assess the prolonged gastric retention of the formulations. 99mTc–Ofloxacin served as a good tracer for studying the pharmacokinetics of three controlled release mucoadhesive dosage forms by gamma scintigraphy studies.

Clinical and ultrasound features of congenital hypothyroidism

Congenital hypothyroidism is a condition where a newborn has decreased or absent thyroid function and thyroid hormone production. It is the most common cause of preventable mental retardation and its early diagnosis can only be achieved through systematic neonatal screening because its clinical manifestations are usually late. The etiologic study of this condition relies heavily on nuclear medicine and ultrasound, describing various findings. This research analyzed the characteristics of the ultrasound patterns observed in these children and their correlation with the most common etiologies. The use of ultrasound allows selecting children that require scintigraphic studies, decreasing the use of radiation in neonates.

A novel gastroretentive porous microparticle for anti-Helicobacter pylori therapy: Preparation, in vitro and in vivo evaluation

Gastroretentive drug delivery system is a promising option for the treatment of Helicobacter pylori infection, which can prolong gastric residence time and supply high drug concentration in the stomach. In the present study, a low density system of metronidazole-loaded porous Eudragit® RS microparticle with high drug loading capacity (>25%) was fabricated via electrospray method. The porous structure and size distribution of microparticles were affected by polymer concentration and flow rate of solution. FTIR and XRD analyses indicated that drug has been entrapped into the porous microparticles. In addition, sustained release profiles and slight cytotoxicity in vitro were detected. Gamma scintigraphy study in vivo demonstrated that ¹³¹I-labeled microparticles retained in stomach for over 8h, and about 65.50% radioactive counts were finally detected in the region of interest. The biodistribution study confirmed that hotspot of radioactivity was remaining in the stomach. Furthermore, metronidazole-loaded porous microparticles can eradicate H. pylori completely with lower dose and administration frequency of antibiotic compared with pure drug, which were also more helpful for the healing of mucosal damages. These results suggest that prepared porous microparticle has the potential to provide better treatment for H. pylori infection.

Foster®: A High-Efficiency Combination Metered Dose Inhaler with Consistent Particle Size Distribution at Alternative Flow Rates

This publication adds perspective to a recent publication by Johal et al. that presented the performance of combination inhalation therapies at a flow rate differing from that recommended by the regulatory authorities for metered dose inhaler (MDI) performance testing. Altering the flow rate through an impactor can create potential pitfalls which can result in performance misrepresentation. In-house data for Foster® (Chiesi, Parma, Italy) and Flutiform® (Bard Pharmaceuticals Limited, Cambridge, UK) have been collected using standard pharmacopaeial conditions and also at the unconventional 60 L/min flow rate utilized by Johal et al. A marked reduction in mass median aerodynamic diameters (MMADs) of both the inhaled corticosteroids (ICS) and long-acting beta agonists in Foster MDI from approximately 1.2–0.5 μm with increase in flow rate (Johal et al.) is not observed. Use of the Andersen cascade impactor at flow rates above 28.3 L/min is not common practice. The industry generally utilizes data from the next generation impactor (NGI), an impactor specifically designed and developed for this purpose. Data for the ICS component of Foster have been generated using an NGI operated at 30 and 60 L/min, yielding an MMAD (±SD) of 1.1 ± 0.1 μm at both flow rates. Johal et al. suggest that submicron particles are prone to be exhaled by the patient, and therefore imply that they may be non-effective. However, therapeutic significance of submicron particles is supported by a scintigraphic lung deposition study carried out using the Foster MDI. The in vivo data highlight that just 2–3% of the nominal dose was exhaled, with 31–34% deposited in the lungs. Consistent particle size distribution of both active drug components delivered from Foster MDI at flow rates of 28–30 and 60 L/min is observed.

Diagnostic performance of IAEA software package for the analysis of scintigraphic renal dynamic studies: Preliminary results for semi-quantitative parameters of technetium-99m mercapto-acetyltriglycine renogram in healthy individuals

The aims of this study in healthy individuals were: a) to implement the International Atomic Energy Agency (IAEA) Software Package into analysis of technetium-99m mercapto-acetyltriglycine (99mTc MAG3) dynamic scintigraphy, b) to validate results of renogram parameters against their reference values, and c) to compare different renogram indices of kidney excretion in order to assess whether the clinical information provided by all of them is identical. Study population consisted of 20 healthy subjects who were evaluated by 99mTc MAG3 dynamic scintigraphy for kidney donation. The IAEA software was applied to process the studies. The parameters analyzed were: time to maximum activity (Tmax), time to half maximum (T1/2) of the curves, normalized residual activity at 20 minutes (NORA 20), output efficiency at 20 minutes (OE 20), residual activity (RA), elimination index (EI), whole kidney mean transit time (MTT), mean parenchymal transit time (MPTT) and relative kidney function (RF). Correspondence between OE 20, NORA 20, RA and EI was evaluated by Pearson correlation coefficient and linear regression analysis. The results for normal kidneys were presented as follows: Tmax: 3.4+0.7 min; T1/2:6.1+1.5min; NORA20:0.34+0.09;OE20: 93+2.2%; RA: 26+6.2%; EI: 2.2+0.4; MTT: 2.+0.4 min and MPTT: 1.7+0.4 min. Relative function for the left and right kidney was 52% and 48%+.4%, respectively. The excellent agreement was observed between the obtained values of renogram parameters and their reference values. Significant linear correlation between parameters of kidney excretion was obtained. The highest correlation was observed between NORA 20 and OE 20 (r=-0.936, p&lt; 0.01). In Conclusion, the IAEA Software gives reliable values of numerical parameters of kidney excretion. Results obtained for normal kidneys were almost identical with previously reported reference values for MAG3 parameters. Only the results for MTT and MPTT were systematically lower than the established normal values. NORA 20 highly corresponds with OE 20 and could replace the former parameter in the evaluation of kidney drainage. The preliminary results support the wide-spread use of IAEA software package in order to standardize the technique of dynamic renal scintigraphy.

Lacrimal outflow mechanisms and the role of scintigraphy: current trends.

Lacrimal outflow can be compromised by anatomical obstructions or stenoses (nonfunctional epiphora) or by defective lacrimal “pump” function (functional epiphora). Although classic imaging modalities, such as X-ray dacryocystography, computed tomography, or magnetic resonance imaging can effectively evaluate the former, their success is much less in the evaluation of the latter. This is largely due to the fact that forced diagnostic injection of fluid into the canalicular system can overcome partial obstruction sites. On the other hand, lacrimal scintigraphy mimicks “physiological” lacrimal outflow, being performed under pressure gradients present in everyday life. This is why it is considered more suitable for the study of functional epiphora. Furthermore, quantitative lacrimal scintigraphy (with time-activity curves) enables the accurate measurement of lacrimal clearance from the conjunctival fornices and may be used to study the physiology of the lacrimal “pump.” Data obtained from the scintigraphic study of lacrimal outflow may be used to design more effective procedures in the management of functional and nonfunctional epiphora. This is a review article, based on a literature search with emphasis on recent publications and on those supporting interdisciplinary cooperation between ophthalmology and nuclear medicine.

Regional deposition of mometasone furoate nasal spray suspension in humans.

Nasal deposition studies can demonstrate whether nasal sprays treating allergic rhinitis and polyposis reach the ciliated posterior nasal cavity, where turbinate inflammation and other pathology occurs. However, quantifying nasal deposition is challenging, because in vitro tests do not correlate to human nasal deposition; gamma scintigraphy studies are thus used. For valid data, the radiolabel must distribute, as the drug, into different-sized droplets, remain associated with the drug in the formulation after administration, and not alter its deposition. Some nasal deposition studies have demonstrated this using homogenous solutions. However, most commercial nasal sprays are heterogeneous suspensions. Using mometasone furoate nasal suspension (MFS), we developed a technique to validate radiolabel deposition as a surrogate for nasal cavity drug deposition and characterized regional deposition and nasal clearance in humans. Mometasone furoate (MF) formulation was spiked with diethylene triamine pentacaetic acid. Both unlabeled and radiolabeled formulations (n = 3) were sprayed into a regionally divided nasal cast. Drug deposition was quantified by high pressure liquid chromatography within each region; radiolabel deposition was determined by gamma camera. Healthy subjects (n = 12) were dosed and imaged for six hours. Scintigraphic images were coregistered with magnetic resonance imaging scans to quantify anterior and posterior nasal cavity deposition and mucociliary clearance. The ratio of radiolabel to unlabeled drug was 1.05 in the nasal cast and regionally appeared to match, indicating that in vivo radiolabel deposition could represent drug deposition. In humans, MFS delivered 86% (9.2) of metered dose to the nasal cavity, approximately 60% (9.1) of metered dose to the posterior nasal cavity. After 15 minutes, mucociliary clearance removed 59% of the initial radiolabel in the nasal cavity, consistent with clearance rates from the ciliated posterior surface. MFS deposited significant drug into the posterior nasal cavity. Both nasal cast validation and mucociliary clearance confirm the radiolabel deposition distribution method accurately represented corticosteroid nasal deposition.

Evaluation Bone Uptake of Alendronate Sodium Via Vaginal Route by Gamma Scintigraphy, Vaginal Uptake of Alendronate Sodium

Alendronate sodium (ALD) is a second generation amino bisphosphonate that use for treatment of bone diseases. Since ALD is poorly absorbed from the gastrointestinal tract and its absorption is markedly reduced by food, the aim of this study is to evaluate the bone uptake of ALD through vaginal route. To evaluate the bone uptake of ALD by gamma scintigraphy, ALD was radiolabeled with Technetium-99 m ( 99m Tc). Vaginal supposi-tories and injectable solution of 99m Tc-ALD was prepared and gamma scintigraphy studies were performed with intravaginally and intravenously 99m Tc-ALD applied rabbits. The results were revealed that ALD was successfully labeled with 99m Tc. After intravaginal and intravenous application, 99m Tc-ALD showed a high uptake in bone. Despite accumulation times and uptake ratios showed differences between administration routes, our preliminary observations suggest that the intravaginal route appears to be a viable alternative for ALD application and should be evaluated in future clinical studies.

Formulation, evaluation and optimization of pectin- bora rice beads for colon targeted drug delivery system.

The purpose of this research was to established new polysaccharide for the colon targeted drug delivery system, its formulation and in vitro and in vivo evaluation. Microspheres containing pectin and bora rice were prepared by ionotropic gelation technique using zinc acetate as cross linking agent and model drug used was glipizide. A 3(2) full factorial design was employed to study the effect of independent variables, polymer to drug ratio (A), and concentration of cross linking agent (B) on dependent variables, particle size, swelling index, drug entrapment efficiency and percentage drug release. RESULTS of trial batches indicated that polymer to drug ratio and concentration of cross linking agent affects characteristics of beads. Beads were discrete, spherical and free flowing. Beads exhibited small particle size and showed higher percentage of drug entrapment efficiency. The optimized batch P2 exhibited satisfactory drug entrapment efficiency 68% and drug release was also controlled for more than 24 hours. The polymer to drug ratio had a more significant effect on the dependent variables. In vivo gamma scintigraphy study of optimized pectin-bora rice beads demonstrated degradation of beads whenever they reached to the colon. Bora rice is potential polysaccharide for colon targeted drug delivery system.