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Synthesis of cephradine metal complexes and its anti-bacterial evaluation

Iqbal Hussain, Syed Salman, Sarwat Iftikhar, Samin Jan, Junaid Akhter, Muhammad Ramzan, et al.

Sains Malaysiana, 2018;47:749-754.

Cephradine belongs to the first generation cephalosporin having a broad range of anti-bacterial activities. In the
present work, Cephradine wasreacted with different metal salts. These metal salts were Iron, Copper, Cobalt and Nickel
salts. All the complexes of Cephradine metals were synthesized at room temperature using a mechanical vibrator.
The reactions yielded the coordinated complexes within 5-10 min with improved product yield. The synthesized
complexes were analyzed for their antibacterial power using disc diffused assay. All the Cephradine complexes showed
powerful antibacterial activity. The Co, Cu, Ni and Sn complexes showed good antibacterial activities 18.5 mm by Cu
complexes against S. typhi, 17 mm against B. subtillus 16.5 mm against S. aureus, 16 mm against S. coccus. Similarly
Sn complexes exhibited 17 mm zone of inhibition against S. coccus and 15.5 mm against B. subtillus. Cobalt and Ni
complexes also shed significant inhibition activities against bacterial pathogenic bacterial strains. The study is of
particular importance and new, using mechanical vibrator for the first time. The product yield is also comparatively
good with short reaction time.
Fulltext A new strategy for taste masking of azithromycin antibiotic: development, characterization, and evaluation of azithromycin titanium nanohybrid for masking of bitter taste using physisorption and panel testing studies

Amin F, Khan S, Shah SMH, Rahim H, Hussain Z, Sohail M, et al.

Drug Des Devel Ther, 2018;12:3855-3866.
PMID: 30510401 DOI: 10.2147/DDDT.S183534

Background: The obnoxious bitter taste of orally taken antibiotics is one of the biggest problems in the treatment of children. The pediatric population cannot tolerate the bitter taste of drugs and vomit out which ultimately leads to suboptimal therapeutic value, grimace and mental stress so it is the challenging task for the formulation scientists to formulate a palatable formulation particularly to overcome address the issue.
Purpose of study: The study aimed to mask and evaluate the unpleasant bitter taste of azithro-mycin (AZ) in the dry suspension dosage form by physisorption technique.
Materials and methods: AZ was selected as an adsorbent and titanium dioxide nanoparticles as adsorbate. The AZ nanohybrids (AZN) were prepared by treating fixed amount of adsorbent with a varied amount of adsorbate, prepared separately by dispersing it in an aqueous medium. The mixture was sonicated, stirred followed by filtration and drying. The AZN produced were characterized by various techniques including scanning electron microscopy (SEM), energy dispersive X-rays (EDX), powder X-ray diffraction (PXRD), HPLC and Fourier-transformed infrared (FTIR). The optimized nanohybrid was blended with other excipients to get stable and taste masked dry suspension dosage form.
Results: The results confirmed the adsorption of titanium dioxide nanoparticles on the surface of AZ. The fabricated optimized formulation was subjected for taste masking by panel testing and accelerated stability studies. The results showed a remarkable improvement in bitter taste masking, inhibiting throat bite without affecting the dissolution rate. The product showed an excellent stability both in dry and reconstituted suspension. The optimized formulation of AZN and was found stable when subjected to physical and chemical stability studies, this is because of short and single step process which interns limits the exposure of the product to various environmental factors that could potentially affect the stability of the product. The dissolution rate of the optimized formulation of AZN was compared with its marketed counterpart, showing the same dissolution rate compared to its marketed formulation.
Conclusion: The current study concludes that, by fabricating AZ-titanium nanohybrids using physisorption can effectively mask the bitter taste of the drug. The palatability and stability of azithromycin formulation was potentially enhanced without affecting its dissolution rate.
Fulltext Experimental and molecular modeling approach to optimize suitable polymers for fabrication of stable fluticasone nanoparticles with enhanced dissolution and antimicrobial activity

Ahmed S, Govender T, Khan I, Rehman NU, Ali W, Shah SMH, et al.

Drug Des Devel Ther, 2018;12:255-269.
PMID: 29440875 DOI: 10.2147/DDDT.S148912

Background and aim: The challenges with current antimicrobial drug therapy and resistance remain a significant global health threat. Nanodrug delivery systems are playing a crucial role in overcoming these challenges and open new avenues for effective antimicrobial therapy. While fluticasone (FLU), a poorly water-soluble corticosteroid, has been reported to have potential antimicrobial activity, approaches to optimize its dissolution profile and antimicrobial activity are lacking in the literature. This study aimed to combine an experimental study with molecular modeling to design stable FLU nanopolymeric particles with enhanced dissolution rates and antimicrobial activity.
Methods: Six different polymers were used to prepare FLU nanopolymeric particles: hydroxyl propyl methylcellulose (HPMC), poly (vinylpyrrolidone) (PVP), poly (vinyl alcohol) (PVA), ethyl cellulose (EC), Eudragit (EUD), and Pluronics®. A low-energy method, nanoprecipitation, was used to prepare the polymeric nanoparticles.
Results and conclusion: The combination of HPMC-PVP and EUD-PVP was found most effective to produce stable FLU nanoparticles, with particle sizes of 250 nm ±2.0 and 280 nm ±4.2 and polydispersity indices of 0.15 nm ±0.01 and 0.25 nm ±0.03, respectively. The molecular modeling studies endorsed the same results, showing highest polymer drug binding free energies for HPMC-PVP-FLU (-35.22 kcal/mol ±0.79) and EUD-PVP-FLU (-25.17 kcal/mol ±1.12). In addition, it was observed that Ethocel® favored a wrapping mechanism around the drug molecules rather than a linear conformation that was witnessed for other individual polymers. The stability studies conducted for 90 days demonstrated that HPMC-PVP-FLU nanoparticles stored at 2°C-8°C and 25°C were more stable. Crystallinity of the processed FLU nanoparticles was confirmed using differential scanning calorimetry, powder X-ray diffraction analysis and TEM. The Fourier transform infrared spectroscopy (FTIR) studies showed that there was no chemical interaction between the drug and chosen polymer system. The HPMC-PVP-FLU nanoparticles also showed enhanced dissolution rate (P<0.05) compared to the unprocessed counterpart. The in vitro antibacterial studies showed that HPMC-PVP-FLU nanoparticles displayed superior effect against gram-positive bacteria compared to the unprocessed FLU and positive control.
Occupational and patients effective radiation doses in dental imaging

Tamam N, Almuqrin AH, Mansour S, Elnour A, Musa M, Omer H, et al.

Appl Radiat Isot, 2021 Nov;177:109899.
PMID: 34438276 DOI: 10.1016/j.apradiso.2021.109899

Ionizing radiation exposure from medical applications is increasing annually worldwide. It was estimated that 325 million dental procedures were performed in the United States. Radiation exposure from dental radiography consists of intraoral, panoramic, and 3D imaging cone-beam computed tomography (CBCT) imaging. Recent studies reported an association between dental imaging procedures and increased cancer probability of brain and thyroid. Previous studies showed that some dental imaging practices exposed patients and staff to unnecessary radiation doses due to incorrect image acquisition and insufficient radiation protection measures. This study aims to (i) measure the occupational and patients doses during dental procedures and (ii) assess the current imaging techniques and radiation protection practices. Two hundred fourteen patients were evaluated for periapical, bitewing, cephalometric, occlusal, and panoramic procedures. Organ equivalent doses were quantified for the breast, eye lens, and thyroid gland during CBCT procedure. Occupational and ambient dose assessment were assessed using calibrated thermoluminescent dosimeters (TLD-100(LiF: Mg. Ti). Ambient doses were measure at different locations at the department using TLDs. Patients' radiation doses were quantified using kerma area product (PKA (mGy.cm) and the entrance surface air kerma (ESAK (mGy). Fixed tube voltage (65 kVp) and tube current-time product (7 mAs) were used. The overall mean, sd, and range of patients dose values during intraoral (mGy), panoramic and CBCT examinations were 4.6 ± 0.7 (1.4-7.1), 135 ± 45 (75.2-168.5), and 215 ± 165 (186-2115), respectively. The mean and range of the annual occupational doses (mSv) were 1.4 (0.6-3.7), which below the annual dose limits for radiation workers (20 mSv/y). The study showed that inadequate radiation protection for patients existed in terms of the use of the thyroid shield, the technologist's presence inside the room during radiation exposure. Patients' radiation doses were comparable with the international diagnostic reference level (DRL). Staff education and training in radiation protection aspects are highly recommended.