Polymeric films composed of mixture of ethyl cellulose (EC) and hydroxypropyl cellulose (HPC) are prepared from casting combined solvent (methylene chloride and methanol in 1:1 ratio) containing 8% weight/volume of both polymers (EC to HPC in 1:3 weight ratio). The structural and optical studies of the films are carried out by X-ray diffraction and UV–vis spectrophotometer. The films are polycrystalline structure with an average grain size from 23.15 to 10.79 nm. The possible optical transition in these films is found to be allowed direct transition. The optical band gap energy (Eg) is estimated to be 5.02 eV for HPC–EC plain film and then decreases with increasing the filler content reaching to 4.24 eV for the film filled with maximum Se80Te14Sn6 content of 1 w%. This suggests that Se80Te14Sn6, as filler, is a good choice to control the optical properties of HPC–EC blend film.

Polymeric films composed of mixture of ethyl cellulose (EC) and hydroxypropyl cellulose (HPC) are prepared from casting combined solvent (methylene chloride and methanol in 1:1 ratio) containing 8% weight/volume of both polymers (EC to HPC in 1:3 weight ratio). The structural and optical studies of the films are carried out by X-ray diffraction and UV–vis spectrophotometer. The films are polycrystalline structure with an average grain size from 23.15 to 10.79 nm. The possible optical transition in these films is found to be allowed direct transition. The optical band gap energy (Eg) is estimated to be 5.02 eV for HPC–EC plain film and then decreases with increasing the filler content reaching to 4.24 eV for the film filled with maximum Se80Te14Sn6 content of 1 w%. This suggests that Se80Te14Sn6, as filler, is a good choice to control the optical properties of HPC–EC blend film.

The determination of sodium cromoglicate (SCG) and fluorometholone (FLU) in ophthalmic solution was developed by simple, sensitive and precise methods. Three spectrophotometric methods were applied: absorptivity factor (a-Factor method), absorption factor (AFM) and mean centering of ratio spectra (MCR). The linearity ranges of SCG were found to be (2.5–35 µg/mL) for (a-Factor method) and (MCR); while for (AFM), it was found to be (7.5–50 µg/mL). The linearity ranges of FLU were found to be (4–16 µg/mL) for (a-Factor method) and (AFM); while for (MCR), it was found to be (2–16 µg/mL). The mean percentage recoveries/RSD for SCG were found to be 100.31/0.90, 100.23/0.57 and 100.43/1.21; while for FLU, they were found to be 100.11/0.56, 99.97/0.35 and 99.94/0.88 using (a-Factor method), (AFM) and (MCR), respectively. A TLC-spectrodensitometric method was developed by separation of SCG and FLU on silica gel 60 F254 using chloroform : methanol : toluene : triethylamine in the ratio of (5:2:4:1 v/v/v/v) as developing system, followed by spectrodensitometric measurement of the bands at 241 nm. The linearity ranges and the mean percentage recoveries/RSD were found to be (0.4–4.4 µg/band), 100.24/1.44 and (0.2–1.6 µg/band), 99.95/1.50 for SCG and FLU, respectively. A comparative study was conducted between the proposed methods to discuss the advantage of each method. The suggested methods were validated in compliance with the ICH guidelines and were successfully applied for the determination of SCG and FLU in their laboratory prepared mixtures and commercial ophthalmic solution in the presence of benzalkonium chloride as a preservative. These methods could be an alternative to different HPLC techniques in quality control laboratories lacking the required facilities for those expensive techniques.

Three simple, sensitive, and specific methods were developed for simultaneous determination of amlodipine besylate (AML) and Perindopril Erbumine (PER) without previous separation. The first method was dependent on the first derivative of the ratio spectra by measuring the amplitudes at 348 nm for amlodipine using 50 µg mL1 of perindopril as a divisor and at 227 nm for perindopril using 30 µg mL1 of amlodipine as a divisor. The second method was based on ion-pair RP-HPLC. Satisfactory resolution was achieved using RP-C18 chromatographic column Zorbax Extend column and a mobile phase consists of potassium dihydrogen phosphate buffer (0.05 M, pH 3.00.02 adjusted by orthophosphoric acid): acetonitrile 30:70 v/v at a flow rate 1 mL/min using 0.002 M sodium heptanesulfonate in the aqueous phase. UV detection was performed at 215 nm. The third method was based on TLC; the separation was carried out on Fluka TLC aluminum sheets silica gel 60 F254, using n-butanol : water : glacial acetic acid (4:5:1, v/v/v) as the mobile phase. The validation of the proposed methods was applied according to ICH guidelines and LOD and LOQ were calculated. The suggested methods were successfully applied for the determination of the cited drugs in bulk powder and commercial tablets.

Aim: To conduct a comparative study between the smart novel ratio difference spectrophotometric method (RDSM) versus four spectrophotometric methods: first derivative spectrophotometry (D1), first derivative of the ratio spectra (1DD), isoabsorpative point (Aiso), ratio subtraction (RS), and two chemometric techniques based on principal component regression (PCR) and partial least-squares (PLS-1) for the determination of a binary mixture of Ofloxacin (OFX) and Dexamethasone (DXM). Study Design: The results obtained from the proposed methods were statistically compared to the reported HPLC method using student’s t-test, F-test and One way ANOVA. Methodology: (OFX) was determined by the application of direct spectrophotometry, by measuring its zero-order (D0) absorption spectra at its λmax = 296.6 nm. (DXM) was determined by (D1) at 227.1 nm. By applying (1DD), (DXM) was determined at 237.3. The total concentration of both (OFX + DXM) was determined at their isoabsorpative point λiso= 238.3 nm, then the concentration of (DXM) in mixtures were calculated by subtraction. (DXM) was determined using the (RS) method at its λmax = 239 nm. (DXM) was determined using (RDSM) by measuring amplitude difference at two selected wavelengths (248.4 and 290 nm). A concentration of 10 μg.mL1 of OFX was used as a divisor. The linearity range was found to be (1-10 μg.mL1) and (2-14 μg.mL1) for OFX and DXM respectively. Results: The recovery percentage for OFX was found to be 100.07 ± 0.65 and for DXM was found to be 100.41 ± 0.84, 100.15 ± 0.97, 100.14 ± 0.91, 100.54 ± 0.75 and 100.11 ± 0.66 for the five methods, respectively. Conclusion: The novel method showed advantages over the other proposed methods regarding simplicity, minimal data manipulation and maximum reproducibility and robustness; which enabled the analysis of binary mixtures with overlapped spectra for routine quality control testing with quite satisfactory and in lower cost.

Aims: Topical drug delivery of fluconazole, an antifungal drug, in gel form was formulated to avoid the side effect of the oral route. Study Design: In this study I prepare different formulation from different polymers and select the best formulation to undergo further antifungal and stability studies. Place and Duration of Study: Faculty of Pharmacy, Department of Pharmaceutics, Assiut University, between May 2010 and July 2011. Methodology: Different polymers; Sodium carboxymethyl cellulose, Sodium alginate, Carbopol 934P, Hydroxypropylmethyl cellulose, Pluronic F-127 and hydroxypropyl cellulose, were used. The compatibility of fluconazole and different gelling polymer was assessed through differential scanning calorimetry and infrared absorption spectroscopy. The influence of polymer type and concentration on fluconazole release from the prepared gels were studied. The prepared gel formulations were evaluated for pH, drug content, rheology, spreadability and in vitro drug release. Results: The rheological behavior of all the prepared gels showed a pseudoplastic flow (shear thinning) which is a good characteristic in the pharmaceutical gels. With the increase of the polymer concentration in the formulation, viscosity increased and in vitro release of fluconazole decreased. Among all the prepared formulations, 0.5% Carbopol 934P gel showed desired properties and exhibited the best fluconazole in vitro release that reaches 77% over a 3-hr period. This gel showed a good inhibition to the fungal growth against Candida albicans and Trichophyton mentagrophyte using cup plate method and also, showed good stability. Conclusion: 0.5% Carbopol 934P / Fluconazole gel is a promising dosage form for the treatment of superficial fungal infections and could be used for further clinical studies.

Aims: Topical drug delivery of fluconazole, an antifungal drug, in gel form was formulated to avoid the side effect of the oral route. Study Design: In this study I prepare different formulation from different polymers and select the best formulation to undergo further antifungal and stability studies. Place and Duration of Study: Faculty of Pharmacy, Department of Pharmaceutics, Assiut University, between May 2010 and July 2011. Methodology: Different polymers; Sodium carboxymethyl cellulose, Sodium alginate, Carbopol 934P, Hydroxypropylmethyl cellulose, Pluronic F-127 and hydroxypropyl cellulose, were used. The compatibility of fluconazole and different gelling polymer was assessed through differential scanning calorimetry and infrared absorption spectroscopy. The influence of polymer type and concentration on fluconazole release from the prepared gels were studied. The prepared gel formulations were evaluated for pH, drug content, rheology, spreadability and in vitro drug release. Results: The rheological behavior of all the prepared gels showed a pseudoplastic flow (shear thinning) which is a good characteristic in the pharmaceutical gels. With the increase of the polymer concentration in the formulation, viscosity increased and in vitro release of fluconazole decreased. Among all the prepared formulations, 0.5% Carbopol 934P gel showed desired properties and exhibited the best fluconazole in vitro release that reaches 77% over a 3-hr period. This gel showed a good inhibition to the fungal growth against Candida albicans and Trichophyton mentagrophyte using cup plate method and also, showed good stability. Conclusion: 0.5% Carbopol 934P / Fluconazole gel is a promising dosage form for the treatment of superficial fungal infections and could be used for further clinical studies.

Magnetic nanoparticles that are currently explored for various biomedical applications exhibit a high propensity to minimize total surface energy through aggregation. This study introduces a unique, thermoresponsive nanocomposite design demonstrating substantial colloidal stability of superparamagnetic Fe3O4 nanoparticles (SPIONs) due to a surface-immobilized lipid layer. Lipid coating was accomplished in different buffer systems, pH 7.4, using an equimolar mixture of 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and L-α-dipalmitoyl-phosphatidyl glycerol (DPPG). Particle size and zeta potential were measured by dynamic laser light scattering. Heating behavior within an alternating magnetic field was compared between the commercial MFG-1000 magnetic field generator at 7 mT (1 MHz) and an experimental, laboratory-made magnetic hyperthermia system at 16.6 mT (13.7 MHz). The results revealed that product quality of lipid-coated SPIONs was significantly dependent on the colloidal stability of uncoated SPIONs during the coating process. Greatest stability was achieved at 0.02 mg/mL in citrate buffer (mean diameter = 80.0 ± 1.7 nm; zeta potential = −47.1 ± 2.6 mV). Surface immobilization of an equimolar DPPC/DPPG layer effectively reduced the impact of buffer components on particle aggregation. Most stable suspensions of lipid-coated nanoparticles were obtained at 0.02 mg/mL in citrate buffer (mean diameter = 179.3 ± 13.9 nm; zeta potential = −19.1 ± 2.3 mV). The configuration of the magnetic field generator significantly affected the heating properties of fabricated SPIONs. Heating rates of uncoated nanoparticles were substantially dependent on buffer composition but less influenced by particle concentration. In contrast, thermal behavior of lipid-coated nanoparticles within an alternating magnetic field was less influenced by suspension vehicle but dramatically more sensitive to particle concentration. These results underline the advantages of lipid-coated SPIONs on colloidal stability without compromising magnetically induced hyperthermia properties. Since phospholipids are biocompatible, these unique lipid-coated Fe3O4 nanoparticles offer exciting opportunities as thermoresponsive drug delivery carriers for targeted, stimulus-induced therapeutic interventions.

Objectives: The purpose of this study was to formulate and characterize metoclopramide solid lipid nanoparticles (MCP-SLNs) and incorporating it into suppository bases for treatment of nausea and vomiting, produced with chemotherapeutic agents, using one dose per day. Methods: MCP-SLNs was prepared using high shear homogenization (hot homogenization) technique using different surfactants (tween 80, poloxamer 407, poloxamer 188 and cremophore) in two different concentrations (2.5% and 5%) then solid lipid nanoparticle (SLN), whose release percentage above 50%, was incorporated into suppository for treatment of nausea and vomiting. The prepared SLN and suppositories were then evaluated and characterized. Key findings: Formulation of poloxamer 407 with compritol and drug (F9) produced highest in-vitro % release (80%). Transmission electron microscopy showed that SLN had round and spherical shape in form of solid dispersion or drug-enriched core. Particle size analysis of SLN showed a size range of 24.99–396.8 nm. Negative zeta potential proves complete drug entrapment. In-vivo study of MCP-SLN suppositories produced the same %GE as the market metoclopramide (MCP) suppository (Primperan) with sustained release effect. Conclusion: MCP-SLN suppositories (formula F) can reverse decrease in %GE because of emesis with sustained release effect. So it succeeded to be an alternative to MCP suppositories with no multiple dosing.

Betamethasone sodium phosphate is a potent glucocorticoid with anti-inflammatory activity and can be used in treatment of macular edema. The aim of this work is to formulate and investigate mucoadhesive chitosan-sodium alginate nanoparticles as new vehicle for the prolonged topical ophthalmic delivery of betamethasone sodium phosphate. Ionotropic gelation method was used to produce betamethasone loaded chitosan alginate nanoreservoir system. The effect of changing different formulation parameters (pH of chitosan solution, sodium alginate concentration, calcium chloride concentration, chitosan concentration, drug concentration and the addition of tween 80) on the physicochemical properties and in-vitro release of the drug loaded nanoparticles was studied. The mean particle size ranged from 16.8 to 692 nm and the zeta potential generally ranged from +18.49 to +29.83 mV depending on the formulation conditions. The highest encapsulating efficiency obtained was 64%. In-vitro release studies showed an initial burst release of the drug followed by slow sustained release over 24, 48 or 72 hours depending on the formulation parameters. The in-vivo studies carried out for two selected formulations showed the release of 84%, 59.5% of the drug over 12 hours for both F3C and F12 respectively. The results of physicochemical properties of F3C and F12 upon storage showed good stability at both 25°C and 40°C as the drug content was within the accepted range, the pH was (5–7) and the mean particle size for both formulations over the three months was still interesting for ophthalmic application. The results of this study suggest that chitosan alginate nanoparticles would be a promising system for the sustained release delivery of betamethasone sodium phosphate to the posterior segment of the eye.