2^nd International Conference on Pharmaceutical Research & Innovations in Pharma Industry May 30-31, 2019 | Orlando, Florida, USA

Some of the drugs get absorbed from a particular absorption site in the GI tract i.e., they have absorption window like stomach or upper part of the intestine. These drugs do not get absorbed completely when administered in the form of a typical controlled drug delivery system. Gastro-retentive drug delivery systems (GRDDS) can be used as carriers for drugs with a so-called absorption window. It is obtained by retaining dosage form into stomach and drug is being released at controlled manner to the specific site either in stomach, duodenum or intestine. Several gastro-retentive drug delivery approaches being designed and developed including high density system that is retained in the bottom of the stomach, low density (floating) systems that causes buoyancy in gastric fluid, mucoadhesive systems that causes bioadhesion to stomach mucosa, unfoldable, extendible or swellable systems which limits emptying of the dosage form through the pyloric sphincter of stomach, superporous hydrogel systems and magnetic systems etc. Floating drug delivery systems (FDDS) or hydrodynamically controlled systems are lowdensity systems that have sufficient buoyancy to float over the gastric content and remain buoyant in the stomach without affecting the gastric emptying rate for a prolonged period of time. While the system is floating on the gastric contents, the drug is released slowly at the desired rate from the system. Floating tablets of cinnarizine, losartan potassium, famotidine, and norfloxacin were developed. Superporous hydrogels are swellable systems with a pore size greater than 100 microns. These systems instantly swell in the stomach and maintain their integrity in the harsh stomach environment, while releasing the pharmaceutically active ingredient. Supergel hydrogel composite of Zn Carnosine and Cinnarizine were formulated. They were evaluated for their physicochemical characteristics namely floating lag time, total floating time, etc., swelling index and percent drug release.

Beta-lactamases, generally considered the “enemy”, are natural, bacterial-derived enzymes that degrade betalactam antibiotics, confer antibiotic resistance, and dramatically complicate the treatment of bacterial infections. Synthetic Biologics, Inc. has harnessed the potent antibiotic hydrolyzing power of this enzyme class to develop a prophylactic intervention intended to inactivate selected beta-lactam antibiotics in the GI tract to protect the gut microbiome and to prevent the emergence of antimicrobial resistance (AMR). SYN-004, ribaxamase, is intended for use with IV penicillins and cephalosporins. SYN-004, formulated for oral delivery into enteric-coated pellets to protect the enzyme from stomach acid, is released in the upper small intestine at pH>5.5. Animal and human studies demonstrated that ribaxamase degraded antibiotics in the upper GI tract protected the gut microbiome, and reduced AMR. Further examination of this prevention approach, in a phase 2b clinical study, demonstrated that ribaxamase significantly reduced Clostridium difficile infection in high-risk patients who were receiving ceftriaxone for treatment of a lower respiratory tract infection without compromising pulmonary infection control. A new ribaxamase formulation, called SYN-007, was engineered for release in the lower small intestine distal to the site of oral amoxicillin systemic absorption. SYN-007 protected the gut microbiome from damage caused by oral amoxicillin without affecting amoxicillin systemic absorption in dogs. Antibiotic inactivation represents a promising potential new treatment paradigm for the preservation of the gut microbiome and reduction of AMR. SYN-007 is intended to expand beta-lactamasemediated microbiome protection to oral as well as IV beta-lactam antibiotics. 

Introduction: Patellofemoral pain syndrome (PFPS) is the most common presentation of knee pain to sports medicine and orthopaedic clinics among adolescents and young adults. It accounts for 20–40% of all knee problems in active young adults. The purpose of this study was to estimate the prevalence of PFPS in Princess Nourah bint Abdulrahman University (PNU) Students and their impact on their daily activity.

Methods: This study is a crosssectional survey that evaluated 1100 PNU Female students between 18 and 30years of age, who agreed to participate in the study. We used two questionnaires in this study, Kujala Patellofemoral Scale (KPS) and LEFS score.

Results: The average age was 20.7±1.8years, fourteen out of 51 participants with poor/ fair Kujala score aged less than 20years (27.5%), however, no statistically significant association was detected between age and Kujala severity score (p=0.59), using the minimal cut-off of 9 points in LEFS scores showed that all participants had scored 10 and more. Clinically and statistically significant difference in LEFS scores was confirmed among the three Kujala score groups. The higher the Kujala score, the better the LEFS score (r=0.58, p<0.01). 

Purpose: The purpose of this work was to evaluate the antidiarrheal, vasorelaxant, sedative, anxiolytic, and antidepressant actions of tilifodiolide (TFD), a natural diterpene obtained from Salvia tiliifolia Vahl (Lamiaceae).

Methods: The antidiarrheal activity of 1-50mg/kg TFD was assessed with the castor oil test, the charcoal meal test, and the castor oil induced-enteropooling. The relaxation effect of TFD (0.9-298µM) was carried out using smooth muscle tissues from rats, and its mechanism of action was evaluated using different inhibitors involved in muscle relaxation. The sedative, anxiolytic, and antidepressant effects of 1-100mg/kg TFD were calculated with the pentobarbital-induced sleeping time assay, the elevated plus maze test, the light-dark test, the cylinder exploratory test, and the forced swimming test.

Key findings: TFD exhibited anti-diarrheal activity (ED50=10.62mg/kg p.o.) and vasorelaxant effects (EC50=48±3.51µM). The coadministration of TFD with L-NAME or ODQ reverted the vasorelaxant action exposed by TFD alone. TFD exerted anxiolytic activity in all tests and decreased the time of immovability in the forced swimming test. 

Conclusions: TFD exerted antidiarrheal activity by decreasing the intestinal fluid accumulation, and vasorelaxant effects, mediated by NO and cGMP, in isolated aortic rings with intact-endothelium. TFD showed anxiolytic and antidepressant effects in mice. 

Introduction: Ayurveda consists of two words Ayu means ‘life’ or ‘time from birth to death’ and Veda means ‘knowledge’ or ‘learning’. It is an ancient and traditional healthcare system of Indian medicine which has been developed to modern practice as “Tradition to Trend”. The aim of the present project is to combine modern technologies with traditional knowledge of Ayurveda by preparing a liposomal formulation containing gallic acid. The formulations containing Gallic acid available today face problem of rapid elimination from the body. Thus the objective of the project is to incorporate gallic acid into a novel formulation such as liposomes by using phospholipid to prolong its retention time and increase bioavailability as well as the efficacy of the formulation.

Methodology & Theoretical Orientation: Ethanol injection method was used for formulation development of liposomes. After optimization of the process parameters, gallic acid loaded liposomal formulation was successfully developed. The optimized dispersion exhibited enhanced anti-inflammatory activity by carrageenan-induced paw edema method when compared with gallic acid alone. The in-vivo antioxidant activity of gallic acid loaded liposomes showed that the optimized liposomal formulation increased the activity of catalase, superoxide dismutase, reduced glutathione and glutathione peroxidase and decreased the serum level of malondialdehyde.

Conclusion & Significance: The liposomal formulation containing gallic acid was developed successfully and was found to be stable after 3months. The developed liposomal formulation showed statistically significant anti-inflammatory and antioxidant activity as compared to gallic acid alone. Thus, the liposomal formulation is improving the penetration of gallic acid and thus giving enhanced activity.

Acute bacterial pharyngitis is one of the major common diseases accounting for high outpatient visits rates. It is caused by Streptococcus pyogenes (group A betahemolytic); gram-positive cocci containing the Lancefield Group A antigen. Antibiotic prescriptions for pharyngitis have been estimated for increased health costs. It is challenging to distinguish between viral and bacterial pharyngeal infection on sight in outpatient clinics as traditional bacterial pharyngeal identification procedures require almost 24 to 48 hours. However, other approaches as the Rapid Response Strep A Test Strip (RADT) provides results within 5 minutes. The test uses specific antibodies to rapidly, qualitatively and selectively detect the presence of Strep A antigen in throat swab specimens. The study assessed the use of RADT and their impact on antibiotics prescribing behavior of physicians in outpatient clinics in the Ministry of Health hospitals in Alexandria, Egypt. It also studied the barriers hindering the use of RADTs. The study revealed that the physicians’ compliance regarding their use of RADT varied according to their different qualifications’ degrees. Bachelor’s degree physicians were the most to use the RADT resulting in the highest significant decrease in antibiotics prescribing rate from 82.5% to 20% (p=0.002). Followed by master’s degree physicians; they also showed a significant reduction from 92% to 65.7% (p=0.017). A borderline acceptable decline from 86.7% to 80% (p=0.056) was seen among the Ph.D. physicians; they were the least group utilizing RADT as they mainly relied on their clinical experience claiming that the test detects only one bacterium for a positive result, which was considered as the main barrier limiting their use of RADT. However, the study achieved a significant decrease in antibiotics prescription in outpatient clinics attributed to the availability of RADT. Conclusively, RADT could be a reliable tool to ensure bacterial diagnosis through differentiation between viral and bacterial infections. 

This study investigates the effect of a herbal preparation (‘Goko’ Cleanser), on the pharmacokinetic profile of orally administered rifampicin in Swiss albino male rats. The in-vivo study was carried out in three phases. In phase, I only Rifampicin (20mg/kg body) was orally administered to rats and in phase II, rifampicin and Goko Cleanser (30ml/kg body weight) were concurrently administered and in phase III Goko Cleanser was administered for 6 days before Rifampicin. Blood samples were collected from rats in each group at 0, 1, 2, 3, 6, 9 and 12hours in each phase and concentration determined by the spectrophotometric method. Pharmacokinetics parameters determined include Cmax, Tmax, t1/2α, ClT, AUC0-9, AUC 0-∞, t1/2β and kβ. The in-silico studies were done by docking molecules contained in the herbal cleanser into rifampicin binding site on the pregnane X receptor (PXR). The result showed rifampicin pharmacokinetics profile to be in line with previous reports. Goko Cleanser significantly (P<0.05, 0<0.01) increase the Cmax, Tmax, AUC0-9, AUC 0-∞, and t1/2β but decrease ClT, when administering concurrently with Rifampicin (Phase II). Goko Cleanser significantly (P<0.05) decrease the Cmax, Tmax, t1/2α, AUC0-9, AUC 0-∞, and t1/2β but increase ClT when Rifampicin was administered after 6days of taking Goko Cleanser (Phase III). In-silico docking results showed a significant interaction of Goko Cleanser constituents with active site binding residues and complex formation between constituents of Goko cleanser and rifampicin when administered together. Taking herbal preparations such as “Goko cleanser” with rifampicin at the same or within a week should be avoided. 

Background: Spread and emergence of antimalarial drug resistance is the major challenge that endangers all the recent gains in malaria control. Medicinal plants are the key source of new effective antimalarials. Verbascum sinaiticum is commonly used the traditional medicinal plant in many parts of Africa including Ethiopia for treatment of malaria.

Methods: This study attempted to evaluate the in-vivo antimalarial activity of 80% methanol leaf extract of the plant in mice infected with Plasmodium berghei ANKA strain. To this effect, various doses (100, 200, 400mg/kg) of the extract were evaluated for the antimalarial effect using the fourday suppressive, curative and prophylactic tests. Parameters, including percent parasitemia, survival time, body weight, body temperature and packed cell volume (PCV) were determined using standard procedures.

Results: A significant (p<0.001) maximum parasite suppression of 51.34% was observed with 400mg/kg of the extract, in early infection. On the other hand, a significant parasite suppression was observed by the extract in the curative test with 400mg/kg (40.71%, p<0.001) being the highest. In the prophylactic test, 100, 200, and 400mg/kg of the extract produced 23.31%, 39.90% and 61.81% parasite suppression, respectively. In addition, the standard produced significant parasitemia suppression in all tests. In general, the extract has shown considerable invivo antimalarial properties with outstanding prophylactic activity. The phytochemical screening of the extract showed the presence of alkaloids, steroids, tannins, phenols, and flavonoids. The findings suggest that V. sinaiticum contain active phytochemicals that could potentially be a lead compound in the search for new antimalarials. 

Introduction: One of the most popular topical wound treatment is dressing. It can protect wound against the outer environment while preserves a moist wound environment to the wound. Agarose is generally extracted from a natural product that is safe and compatible. Consequently, agarose has been used as a material in drug delivery application including the material in this study. For active ingredient in this dressing, sericin was chosen because sericin is proteins from silk cocoon that can activate fibroblast to promote collagen type I synthesis leading to wound healing promotion.  However, a technology for wound dressing production that is friendly to the environment and costeffectiveness is still limited. The freeze-thawing method is a clean and comfortable method that can process without a special machine. Moreover, it also enhances the physical properties of the wound dressing. Combined the freezethawing process with general wound dressing production may have a good effect on dressing’s mechanical and physical properties. Therefore, the purposes of this study were to fabricate and investigate the properties of agarose dressing containing sericin prepared using the freeze-thawing process combined with freeze-drying method comparing to the pure freeze-drying method.

Methodology: The physical and mechanical properties of the dressing were investigated using Scanning electron microscopy, Fourier-transform infrared spectroscopy and the gel fraction, swelling, releasing, and compressive properties were assessed.

Findings: The mechanical properties of the agarose containing sericin dressing prepared using the freezethawing process combined with the freeze-drying method were superior to those of using the pure freeze-drying method. Moreover, the physical properties of the dressing prepared using the freezethawing process combined with freeze-drying method tended to have better qualities than dressing prepared by pure freeze-drying method. The percentage of swelling of all samples were >90%. Conclusion: The agarose dressing containing sericin prepared using the freezethawing process combined with freeze-drying method seem to be better than pure freeze-drying method. 

Infections caused by multidrugresistant bacteria represent one of the biggest challenges in the medical field. There is an urgent need to develop new antibacterial targets and antibacterial agents to combat multidrug-resistance bacteria. For several years, the main target has been focused on the peptidoglycan biosynthesis pathway which provides a potential route to design novel antibiotic compounds. In fact, most bacteria require either lysine or its biosynthetic precursor, diaminopimelate acid (DAP), as a component of the peptidoglycan layer of the cell wall. Nevertheless, DAP/lysine are not present in mammals, thus, inhibitors of this pathway could provide potential antibacterial agents displaying low mammalian toxicity. In order to fight antibacterial resistance, our work focused on the design and synthesis of new analogs of diaminopimelic acid (DAP) and lysine.

Background and Objectives: Although colistin is a last resort antibiotic, it is applied regularly in animal production. Its increased use may have triggered the emergence of colistin-resistant bacteria. Hence, the aim was to investigate their occurrence in wastewater from poultry and pig slaughterhouses and to examine their emergence after the treatment process in the in-house and municipal wastewater treatment plants (WWTPs). Materials and Methods: Wastewater samples were taken during 2017-2018 along the production chains in two German pig slaughterhouses (n=53) and in its municipal WWTPs (n=36) as well as in two poultry slaughterhouses (n=72). Samples were screened for colistin-resistant bacteria using EMB medium supplemented with 3.5µg/ml colistin sulfate. The final identification was done by MALDI-TOF-MS. Antimicrobial susceptibility tests were performed by the broth microdilution method. Colistinresistant isolates were screened for the presence of colistin resistance genes (mcr 1-5) by PCR. Results: Colistin-resistant bacteria were more abundant in wastewater from the poultry slaughterhouses. Overall, 41.7% of its samples (n=30/72), including the outflows of the in-house WWTP, were found positive. The percentage of positive samples from the pig slaughterhouses and its mWWTPs was lower at 18.0% (n=16/89). Out of 46 samples, a total of 106 colistin-resistant strains were obtained. Among these, the majority belonged to E. coli (39.6%), followed by E. cloacae complex (28.3%), K. pneumoniae (27.4%) and R. ornithinolytica (4.7%). The mcr-1 gene was detected in 69.0% of the E. coli strains (n=29/42), in 13.8% of the K. pneumoniae strains (n=4/29) and in 3.3% of the strains from the E. cloacae complex (n=1/30). Conclusions: Colistin-resistant bacteria were detected in wastewater throughout the production chains as well as in the effluents and preflooder of the in-house and municipal WWTPs. This could pose a threat to human health and needs to be further investigated.