Verapamil hydrochloride (Vp-HCl) is a calcium channel blocker and class IV antiarrythmic drug. Its oral bioavailability is about 20- 30% because of the extensive first-pass metabolism, so it is advisable to prepare the drug in a buccoadhesive dosage forms to bypass first-pass metabolism and thus achieving constant plasma concentrations during treatment of chronic hypertension. Certain bioadhesive polymers were used either singly or in combinations at different ratios in order to select the best matrix forming tablets with satisfactory drug release, characteristic bioadhesiveness and swelling properties. It was found that the drug release decreased by increasing the concentration of the polymer in all the studied formulations and the drug release from using polymer blends is slower than those containing single polymer. Tablet formula containing either 30% (w/w) hydroxypropyl methyl cellulose 15000(HPMC 15000) & 10% (w/w) sodium carboxymethyl cellulose (SCMC), or containing 5% (w/w) carbopol 934P (Cp934P) with either 15% (w/w) HPMC 15000 or 30% (w/w) sodium alginate (NaAlg) was developed to a satisfactory level in terms of drug release, bioadhesive performance and swelling properties. Plasma concentration time curves obtained following buccal administration of the optimal prepared buccoadhesive tablets to rabbits showed evidence of sustained release of Vp-HCl. Bioavailability of Vp-HCl formulated tablets formulae (T31, T35 & T38) was approximately two times higher than that achieved after oral administration of commercial tablets.

Verapamil hydrochloride (Vp-HCl) is a calcium channel blocker and class IV antiarrythmic drug. Its oral bioavailability is about 20- 30% because of the extensive first-pass metabolism, so it is advisable to prepare the drug in a buccoadhesive dosage forms to bypass first-pass metabolism and thus achieving constant plasma concentrations during treatment of chronic hypertension. Certain bioadhesive polymers were used either singly or in combinations at different ratios in order to select the best matrix forming tablets with satisfactory drug release, characteristic bioadhesiveness and swelling properties. It was found that the drug release decreased by increasing the concentration of the polymer in all the studied formulations and the drug release from using polymer blends is slower than those containing single polymer. Tablet formula containing either 30% (w/w) hydroxypropyl methyl cellulose 15000(HPMC 15000) & 10% (w/w) sodium carboxymethyl cellulose (SCMC), or containing 5% (w/w) carbopol 934P (Cp934P) with either 15% (w/w) HPMC 15000 or 30% (w/w) sodium alginate (NaAlg) was developed to a satisfactory level in terms of drug release, bioadhesive performance and swelling properties. Plasma concentration time curves obtained following buccal administration of the optimal prepared buccoadhesive tablets to rabbits showed evidence of sustained release of Vp-HCl. Bioavailability of Vp-HCl formulated tablets formulae (T31, T35 & T38) was approximately two times higher than that achieved after oral administration of commercial tablets.

Antimicrobial peptides (AMP) and cell-penetrating peptides (CPP) are two classes of peptides that share some structural and physicochemical similarities. Antennapedia or penetratin (ANT) is one of the most known CPPs, that was proven to have antimicrobial activity against certain strains of planktonic bacteria. ANT can enter the cells but has no activity against intracellular bacteria. This is attributable to the inability of the peptide to reach bacteria reside within cellular components as well as low delivery efficiency, due to loss of activity by proteolysis and poor specificity. The aim of this work is to develop a formulation that can effectively reach and attack intracellular bacteria. To achieve this goal, ANT was encapsulated in PLGA platform as nanoparticles with the size range of 500-1000 nm, which allows for selective uptake by macrophages where bacteria mostly reside. ANT was loaded with high loading efficiency (12.7%) inspite of high water solubility. ANT-nanoparticles (ANT-NP) had no cytotoxicity on J774a.1 macrophages and were readily taken up by macrophages as confirmed by fluorescence microscopy. Antibacterial activity of ANT-NP remains to be tested against different intracellular bacteria.

Antimicrobial peptides (AMP) and cell-penetrating peptides (CPP) are two classes of peptides that share some structural and physicochemical similarities. Antennapedia or penetratin (ANT) is one of the most known CPPs, that was proven to have antimicrobial activity against certain strains of planktonic bacteria. ANT can enter the cells but has no activity against intracellular bacteria. This is attributable to the inability of the peptide to reach bacteria reside within cellular components as well as low delivery efficiency, due to loss of activity by proteolysis and poor specificity. The aim of this work is to develop a formulation that can effectively reach and attack intracellular bacteria. To achieve this goal, ANT was encapsulated in PLGA platform as nanoparticles with the size range of 500-1000 nm, which allows for selective uptake by macrophages where bacteria mostly reside. ANT was loaded with high loading efficiency (12.7%) inspite of high water solubility. ANT-nanoparticles (ANT-NP) had no cytotoxicity on J774a.1 macrophages and were readily taken up by macrophages as confirmed by fluorescence microscopy. Antibacterial activity of ANT-NP remains to be tested against different intracellular bacteria.

Antimicrobial peptides (AMP) and cell-penetrating peptides (CPP) are two classes of peptides that share some structural and physicochemical similarities. Antennapedia or penetratin (ANT) is one of the most known CPPs, that was proven to have antimicrobial activity against certain strains of planktonic bacteria. ANT can enter the cells but has no activity against intracellular bacteria. This is attributable to the inability of the peptide to reach bacteria reside within cellular components as well as low delivery efficiency, due to loss of activity by proteolysis and poor specificity. The aim of this work is to develop a formulation that can effectively reach and attack intracellular bacteria. To achieve this goal, ANT was encapsulated in PLGA platform as nanoparticles with the size range of 500-1000 nm, which allows for selective uptake by macrophages where bacteria mostly reside. ANT was loaded with high loading efficiency (12.7%) inspite of high water solubility. ANT-nanoparticles (ANT-NP) had no cytotoxicity on J774a.1 macrophages and were readily taken up by macrophages as confirmed by fluorescence microscopy. Antibacterial activity of ANT-NP remains to be tested against different intracellular bacteria.

Antimicrobial peptides (AMP) and cell-penetrating peptides (CPP) are two classes of peptides that share some structural and physicochemical similarities. Antennapedia or penetratin (ANT) is one of the most known CPPs, that was proven to have antimicrobial activity against certain strains of planktonic bacteria. ANT can enter the cells but has no activity against intracellular bacteria. This is attributable to the inability of the peptide to reach bacteria reside within cellular components as well as low delivery efficiency, due to loss of activity by proteolysis and poor specificity. The aim of this work is to develop a formulation that can effectively reach and attack intracellular bacteria. To achieve this goal, ANT was encapsulated in PLGA platform as nanoparticles with the size range of 500-1000 nm, which allows for selective uptake by macrophages where bacteria mostly reside. ANT was loaded with high loading efficiency (12.7%) inspite of high water solubility. ANT-nanoparticles (ANT-NP) had no cytotoxicity on J774a.1 macrophages and were readily taken up by macrophages as confirmed by fluorescence microscopy. Antibacterial activity of ANT-NP remains to be tested against different intracellular bacteria.

A simple colorimetric method for the quantitative detection of two cephalosporins, cefoperazone (CFZ) and cefepime (CPM), has been developed and validated for the application in clinical and quality control laboratories. The method was based on exploiting the reducing properties of cephalosporins due to the 7-aminocephalosporanic acid dihydrothiazine and a β-lactam ring to produce gold (GNPs) or silver (AgNPs) nanoparticles from their corresponding metal solutions. The resulting nanoparticles exhibited surface plasmon resonance signals at 530–550 nm or 430 nm for GNPs or AgNPs, respectively, with an intensity dependent on drug concentration that permits the quantitative analysis. Furthermore, the resulting nanoparticles were characterized using a dynamic light scattering instrument and transmission electron microscopy. Factors influence the reaction, such as the reagents volume, pH, temperature and reaction time, have been studied and optimised. In addition, the study was validated according to the official guidelines and extended to evaluate the antimicrobial activity to assess potential drug degradation during the analysis. Overall, the method developed in this study can be used for the quantitative analysis of CFZ and CPM in pure forms and pharmaceutical preparations with relatively good sensitivity and selectivity as well as, acceptable accuracy and precision.

Bacterial pathogens residing in host macrophages in intracellular infections are hard to eradicate because traditional antibiotics do not readily enter the cells or get eliminated via efflux pumps. To overcome this challenge, we developed a new particle formulation with a size amenable to selective macrophage uptake, loaded with two antibacterial agents - pexiganan and silver (Ag) nanoparticles. Here, pexiganan was loaded in 600 nm poly(lactic-co-glycolic acid) (PLGA) particles (NP), and the particle surface was modified with an iron-tannic acid supramolecular complex (pTA) that help attach Ag nanoparticles. PLGA particles coated with Ag (NP-pTA-Ag) were taken up by macrophages, but not by non-phagocytic cells, such as fibroblasts, reducing non-specific toxicity associated with Ag nanoparticles. NP-pTA-Ag loaded with pexiganan (Pex@NP-pTA-Ag) showed more potent antibacterial activity against various intracellular pathogens than NP-pTA-Ag or Pex@NP (pexigananloaded NP with no Ag), suggesting a collaborative function between pexiganan and Ag nanoparticles. Mouse whole-body imaging demonstrated that, upon intravenous injection, NP-pTA-Ag quickly accumulated in the liver and spleen, where intracellular bacteria tend to reside. These results support that Pex@NP-pTA-Ag is a promising strategy for the treatment of intracellular bacterial infection.

Bacterial pathogens residing in host macrophages in intracellular infections are hard to eradicate because traditional antibiotics do not readily enter the cells or get eliminated via efflux pumps. To overcome this challenge, we developed a new particle formulation with a size amenable to selective macrophage uptake, loaded with two antibacterial agents - pexiganan and silver (Ag) nanoparticles. Here, pexiganan was loaded in 600 nm poly(lactic-co-glycolic acid) (PLGA) particles (NP), and the particle surface was modified with an iron-tannic acid supramolecular complex (pTA) that help attach Ag nanoparticles. PLGA particles coated with Ag (NP-pTA-Ag) were taken up by macrophages, but not by non-phagocytic cells, such as fibroblasts, reducing non-specific toxicity associated with Ag nanoparticles. NP-pTA-Ag loaded with pexiganan (Pex@NP-pTA-Ag) showed more potent antibacterial activity against various intracellular pathogens than NP-pTA-Ag or Pex@NP (pexigananloaded NP with no Ag), suggesting a collaborative function between pexiganan and Ag nanoparticles. Mouse whole-body imaging demonstrated that, upon intravenous injection, NP-pTA-Ag quickly accumulated in the liver and spleen, where intracellular bacteria tend to reside. These results support that Pex@NP-pTA-Ag is a promising strategy for the treatment of intracellular bacterial infection.

Bacterial pathogens residing in host macrophages in intracellular infections are hard to eradicate because traditional antibiotics do not readily enter the cells or get eliminated via efflux pumps. To overcome this challenge, we developed a new particle formulation with a size amenable to selective macrophage uptake, loaded with two antibacterial agents - pexiganan and silver (Ag) nanoparticles. Here, pexiganan was loaded in 600 nm poly(lactic-co-glycolic acid) (PLGA) particles (NP), and the particle surface was modified with an iron-tannic acid supramolecular complex (pTA) that help attach Ag nanoparticles. PLGA particles coated with Ag (NP-pTA-Ag) were taken up by macrophages, but not by non-phagocytic cells, such as fibroblasts, reducing non-specific toxicity associated with Ag nanoparticles. NP-pTA-Ag loaded with pexiganan (Pex@NP-pTA-Ag) showed more potent antibacterial activity against various intracellular pathogens than NP-pTA-Ag or Pex@NP (pexigananloaded NP with no Ag), suggesting a collaborative function between pexiganan and Ag nanoparticles. Mouse whole-body imaging demonstrated that, upon intravenous injection, NP-pTA-Ag quickly accumulated in the liver and spleen, where intracellular bacteria tend to reside. These results support that Pex@NP-pTA-Ag is a promising strategy for the treatment of intracellular bacterial infection.