Oral nano-formulation improves pancreatic islets dysfunction via lymphatic transport for antidiabetic treatment

Type 2 diabetes mellitus (T2DM) therapy is facing the challenges of long-term medication and gradual destruction of pancreatic islet β-cells. Therefore, it is timely to develop oral prolonged action formulations to improve compliance, while restoring β-cells survival and function. Herein, we designed a simple nanoparticle with enhanced oral absorption and pancreas accumulation property, which combined apical sodium-dependent bile acid transporter-mediated intestinal uptake and lymphatic transportation. In this system, taurocholic acid (TCA) modified poly(lactic-co-glycolic acid) (PLGA) was employed to achieve pancreas location, hydroxychloroquine (HCQ) was loaded to execute therapeutic efficacy, and 1,2-dilauroyl-sn-glycero-3-phosphocholine (DLPC) was introduced as stabilizer together with synergist (PLGA-TCA/DLPC/HCQ). In vitro and in vivo results have proven that PLGA-TCA/DLPC/HCQ reversed the pancreatic islets damage and dysfunction, thus impeding hyperglycemia progression and restoring systemic glucose homeostasis via only once administration every day. In terms of mechanism PLGA-TCA/DLPC/HCQ ameliorated oxidative stress, remodeled the inflammatory pancreas microenvironment, and activated PI3K/AKT signaling pathway without obvious toxicity. This strategy not only provides an oral delivery platform for increasing absorption and pancreas targetability but also opens a new avenue for thorough T2DM treatment.

Metformin HCl Oral Preparation Exhibits Anticancer Activity In-vitro in a Human Non-small Cell Lung Tumour Cell Line

@#Introduction: The most common variety of lung cancer is non–small cell lung cancer (NSCLC) accounting for 84% of new cases. Surgery, chemotherapy and radiation are the primary treatment option. Metformin has recently been demonstrated to have an anti-tumour impact on various cancer cells. The goal of this investigation was to determine the growth inhibitory, antiproliferative, cytotoxic, apoptotic and cell cycle arrest properties of metformin HCl oral tablets on the A549 lung carcinoma cell line. Methods: The cells were treated with different dosages of an oral preparation of metformin, with untreated cells used as a control. The Trypan Blue Exclusion Assay was used to determine metformin’s inhibitory and cytotoxic effects. Flow cytometry was used to evaluate apoptosis and cell cycle arrest. Results: In a dose-dependent manner, metformin HCl was able to reduce the viability of treated cells compared to the untreated control. Cell proliferation was considerably inhibited in the treated group with the IC50 dose than in the untreated control group and the IC50 dose showed no cytotoxic effect on L929 cells. Induction of apoptosis and cell cycle arrest was observed in the IC50 dose-treated group by Flow cytometry analysis and data showed metformin oral drug causes early apoptosis and a considerable cell increase in the S phase of the cell cycle. Conclusion: Metformin inhibits cell growth and induces apoptosis and cell cycle arrest in the cell line. A comprehensive proteome examination is required to understand more about the mechanism of action of the oral metformin HCl on cancer cells

Research progress of yeast microcapsules as oral drug delivery carrier / 中国药房

As a natural drug delivery carrier with rough and porous surface and hollow core， yeast microcapsules have good safety， high targeting and high stability， and have excellent application prospects in oral drug delivery systems. Yeast cells can be treated and washed with acid-base and organic solvents to obtain loose and porous yeast microcapsules. Yeast microcapsules can encapsulate drugs through electrostatic interactions， passive diffusion， hydrophobic interaction and other methods. The surface of yeast microcapsules is mainly composed of β-glucan， which can maintain stability in the gastrointestinal environment； it can be recognized by the surface-related receptors of immune cells， thus activating the immune response， and can be transported to the lesion site with the movement of lymphocytes after being ingested. Yeast microcapsules are safe and very suitable for delivering vaccines， anti-inflammatory drugs， and anti-tumor drugs. They can not only achieve oral delivery of the aforementioned drugs， but also enhance drug efficacy and improve drug targeting. In the future， more research on systemic transport mechanisms or the development of more efficient combination drug delivery systems can be carried out to fully exhibit the clinical value of yeast microcapsules.

Advances in the study of peptide drugs in oral drug delivery system / 药学学报

Peptide drugs exhibit an irreplaceable role in clinics due to their high specificity, efficiency and low toxicity. At present, more than 80 peptide drugs have been approved for marketing with global sales exceeding $50 billion in 2019. However, with large molecular weights, high hydrophilicity and instability in digestive tract, oral peptide drugs encounter substantial physiological barriers leading to low oral bioavailability. Therefore, peptide drugs are mostly administered by parenteral routes. Although parenteral delivery of peptide drugs achieves high bioavailability, this is associated with inconvenience and discomfort, even causing severe side effects compared with the oral route possessing a high degree of patient compliance. Therefore, numerous studies concentrate on novel strategies to improve the oral bioavailability of peptide drugs. Some delivery technologies such as Eligen™ and Axcess™ have been successfully applied to the oral dosage form of therapeutic peptides and have accelerated relevant oral formulations for Food and Drug Administration (FDA) approval and clinical treatment. In this review, we focus on the oral peptide delivery, mainly summarizing the progress of recent strategies used to overcome oral barriers and the commercialization applications of related patents, which could facilitate the research and development (R&D) of clinical applications of oral delivery techniques for peptide drugs.

Assessment strategies for drug permeability during drug discovery and development / 药学学报

Permeability is a key factor in the bioavailability of oral drugs. Therefore, in the early stage of drug discovery, accurate and efficient evaluation of drug permeability is essential. The parallel artificial membrane permeability assay (PAMPA) with Caco-2 cells model was used by the industry as early evaluation methods. At present, the Ussing chamber rat model is also widely used. This review summarizes the human data for the in vivo single-pass perfusion technique (Loc-I-Gut) – the gold standard, and then focuses on the basic principles, experimental operation, and efficiency of the three in vitro methods, with correlation to the effective permeability coefficient (Peff) and fractional absorbed (Fa) in man. We provide recommendations for the use of proper permeability methods at different stages in drug discovery and development.

Analysis of technical difficulties and new strategies of oral liquid pharmaceutical preparation for children / 药学学报

With the implementation of the two-child policy and the growing demand for child health, pediatric medication has been arousing widespread social concern. To develop the drugs suitable for children, including new compounds, new specifications and new dosage forms, is urgently required for pharmaceutical researchers. In this review, several technical bottlenecks for pediatric oral liquid preparations, as well as the novel strategies involved in drug nanocrystals, self-microemulsion, ion exchange resin and Pickering emulsion were discussed, which may be benefit to play a theoretical guiding role in the research and development of children's oral liquid formulation.

A Review On Co-Processed Excipients: Current And Future Trend Of Excipient Technology

There is no single-component excipient fulfills all the requisite performance to allow an active pharmaceutical ingredient to be formulated into a specific dosage form. Co-processed excipient has received much more attention in the formulation development of various dosage forms, specially for tablet preparation by direct compression method. The objective of this review is to discuss the emergence of co-processed excipients as a current and future trend of excipient technology in pharmaceutical manufacturing. Co-processing is a novel concept of combining two or more excipients that possess specific advantages that cannot be achieved using a physical admixture of the same combination of excipients. This review article discusses the advantages of co-processing, the need of co-processed excipient, general steps in developing co-processed excipient, limitation of co-processed excipient, technologies used in developing co-processing excipients, co-processed excipients in the literature, marketed products and future trends. With advantages offered by the upcoming newer combination of excipients and newer methods of co-processing, co-processed excipients are for sure going to gain attraction both from academia and pharmaceutical industry. Furthermore, it opens the opportunity for development and use of single multifunctional excipient rather than multiple excipients in the formulation.

Calidad en la administración de medicamentos por sondas enterales de una unidad de cuidados intensivos de México / Quality in drug administration by enteral catheters from an intensive care unit in Mexico / Administração de medicamentos de qualidade por sondas enterais unidade de cuidados intensivos do México

ResumenEl objetivo principal de este trabajo es evaluar la calidad en la administración de medicamentos por sondas enterales por el personal de enfermería de una unidad de cuidados intensivos. Metodología: Estudio observacional, transversal y descriptivo. Se consideró el total de profesionales en enfermería (N=30) de un hospital de alta especialidad. Se estudió las variables conocimiento y cumplimiento. Para evaluar el conocimiento en la administración de fármacos por sondas enterales, se utilizó el instrumento de Amuriza "encuesta de administración de fármacos por sonda". Para evaluar el cumplimiento, se empleó la cédula oficial de administración de medicamentos vía oral del Sistema Nacional de Indicadores de Calidad en Salud. Para obtener del nivel de calidad, se creó un índice ponderado general (IPG) a partir de la suma de los valores estimados obtenidos del porcentaje y la puntuación media del nivel de conocimiento y nivel de cumplimiento. Se analizó los datos a través del programa estadístico SSPS V.21.0. Resultados: El nivel de conocimiento promedio fue deficiente en los participantes, el nivel de cumplimiento fue intermedio en el 77%, el nivel de calidad ponderado fue de 5 puntos estimado como deficiente. Conclusiones: El resultado es contrario a lo establecido en los lineamientos de administración de fármacos por sondas, se sugiere adiestramiento y evaluación constante para la mejora continua. Es indispensable el bien saber y el bien hacer en las intervenciones de enfermería.

SummaryThis work has like main purpose evaluate the quality in drug administration by enteral probes in nurses by an Intensive Care Unit. Methodology: observational, transversal and descriptive study. Considered the total number of nurses (N = 30) a high specialty Hospital. We studied the variables knowledge and compliance. To assess knowledge in the ministration of drugs for probes enteral was used the instrument of Amuriza "Survey of administration of drugs". To assess compliance in the administration of oral medications, used oral drug administration official card of national system of indicators of quality in health. To obtain the quality level, it created a weighted General index (IPG) from the sum of the estimated values retrieved from the percentage and the average of the level of knowledge and level of compliance score. The data were analyzed through the statistical program SPSS v.21.0). Results: Average knowledge level was deficient in the participants, the level of compliance was intermediate in 77%, weighted quality level was 5-point estimated as deficient. Conclusions: The result is contrary to established guidelines for administering drugs by probes, training and constant evaluation for continuous improvement is suggested. It is essential for good to know and do well in nursing interventions.

ResumoO principal objetivo deste estudo é avaliar a qualidade na administração de medicamentos por sondas enterais pela equipe de enfermagem da unidade de cuidados intensivos. Metodologia: observacional, estudo transversal e descritivo. os profissionais de enfermagem Total (n = 30) de um hospital altamente especializada foi considerada. As variáveis estudadas conhecimento e conformidade. Para avaliar o conhecimento nas sonda enteral de entrega de drogas, foi utilizado o instrumento Amuriza "tubo de fornecimento de pesquisa de drogas". Para avaliar o cumprimento, foi utilizado o certificado oficial de entrega de droga oral através do Sistema Nacional de Indicadores de Qualidade de Saúde. Para o padrão, um índice global ponderada (IPG) foi criado a partir da soma dos valores obtidos estimados de percentagem e contagem média de nível de conhecimento e nível de conformidade. Os dados foram analisados utilizando o programa de estatística SSPS V.21.0. Resultados: O conhecimento médio foi de participantes deficientes, o nível de adesão foi intermediário em 77%, o nível de qualidade ponderado foi de 5 pontos estimados como pobres. Conclusões: O resultado é contrária às disposições de diretrizes sondas entrega da droga, formação e é sugerido avaliação constante de melhoria contínua. É essencial sabe muito bem que fazer em intervenções de enfermagem.

Procedural nursing management promotes precise medication of patients in department of rheumatology / 现代临床护理

Objective To explore the effect of the procedural nursing management on nursing quality of hospitalized patients in department of rheumatology. Methods About 267 inpatients were divided into control group (n=125) and experiment group (n=142). The control group received routine medication nursing and the experiment patients were treated with procedural nursing management including implementing medication services and analyzing the factors influencing precise medication and the countermeasures . Result The rate of precise medication in the experiment group was significantly higher than that of the control group ( P<0 . 05 ) . Conclusions The procedural nursing management can promote patient's precise medication so as to ensure the therapeutic effect by medication . It does good for the promotion of medication scientizeation and professionalization .

Progress in oral drug-loaded nano-system / 中国生化药物杂志

Oral drug-loaded nano-system include nano-gel drug delivery system, nano-suspension drug delivery system, nano-particle drug delivery system, liposomes drug delivery system, nano-micelles drug delivery system, alcohol liposoms,nano-framework drug delivery system, nano-emulsions drug delivery system, nano-self assembly drug delivery system.These nano-drug delivery systems can serve as multi-functional drug carriers.They may significantly improve the physicochemical and stabilization and biological properties of the free drug, enhance the therapeutic efficiency and reduce toxic side effects.This paper reviews the recent research progress in oral drug-loaded nano-systems.

Oral Disease-Modifying Therapies for Multiple Sclerosis

Classical multiple sclerosis (MS) treatments using first-line injectable drugs, although widely applied, remain a major concern in terms of therapeutic adherence and efficacy. New oral drugs recently approved for MS treatment represent significant advances in therapy. The oral route of administration clearly promotes patient satisfaction and increases therapeutic compliance. However, these drugs may also have safety and tolerability issues, and a thorough analysis of the risks and benefits is required. Three oral drugs have been approved by regulatory agencies for MS treatment: fingolimod, teriflunomide, and dimethyl fumarate. This article reviews the mechanisms of action, safety, and efficacy of these drugs and two other drugs that have yielded positive results in phase III trials: cladribine and laquinimod.

Research progress on evaluation methods of mouthfeel of oral drug delivery system / 中草药

Mouthfeel is an important part of preparation prescription study in oral drug delivery system. The results of traditional sensory evaluation are limited to individual differences of subjects, and own poor reproducibility. In this paper, some new technologies and evaluation methods were reviewed and commented, mainly including taste, adhesion, mucosal irritation, and grittiness, so as to provide methodology references for ODDS in traditional Chinese medicines and promote its progress.

Application of cell co-culture models in absorption of oral drug / 药学实践杂志

Cell co-culture system can better simulate the inner environment of human body ,predict drug transport and metabolism in intestinal environment and increase the relation between in vitro cell model and integral animal test .In recent years ,co-culture cell model plays an increasingly important role in evaluating the absorption of oral drugs ,which becomes the highlight in the evaluation of drug oral absorption during new drug discovery .This essay summarized co-culture cell model which simulates intestinal environment and their application ,and looked into the future of their application in evaluating oral drug intestinal absorption during oral drug discovery .

Preparation and evaluation of sustained-release solid dispersions co-loading gastrodin with borneol as an oral brain-targeting enhancer

Borneol is a traditional Chinese medicine that can promote drug absorption from the gastrointestinal tract and distribution to the brain. However, stomach irritation may occur when high doses of borneol are used. In the present work, gastrodin, the main bioactive ingredient of the traditional Chinese drug "Tianma" (Rhizoma Gastrodiae) was used as a model drug to explore reasonable application of borneol. Sustained-release solid dispersions (SRSDs) for co-loading gastrodin and borneol were prepared using ethylcellulose as a sustained release matrix and hydroxy-propyl methylcellulose as a retarder. The dispersion state of drug within the SRSDs was analyzed by using scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffractometry. The results indicated that both gastrodin and borneol were molecularly dispersed in an amorphous form. Assay of in vitro drug release demonstrated that the dissolution profiles of gastrodin and borneol from the SRSDs both fitted the Higuchi model. Subsequently, gastric mucosa irritation and the brain targeting of the SRSDs were evaluated. Compared with the free mixture of gastrodin and borneol, brain targeting of SRSDs was slightly weaker (brain targeting index: 1.83 vs. 2.09), but stomach irritation obviously reduced. Sustained-release technology can be used to reduce stomach irritation caused by borneol while preserving sufficient transport capacity for oral brain-targeting drug delivery.

Animal experiment study of silica nanoparticles labeled peptides with 125 I / 中国生化药物杂志

Objective To study whether the silica nanoparticles can be used as a biomacromolecular carrier of oral drugs.Methods Studyed the influence of the amount of calcium ions on nano silica nanoparticles morphology,the encapsulation rate of silica nanoparticles on proteins or peptides in the presence of different calcium ions,the situation of proteins or peptides released from silica nanoparticles,enzymolysis of protein packaged by silica, silica nanoparticles labeled peptides with 125 I released in mice.Results Experiments showed that the synthetic silica nanoparticles packaged with peptides could smoothly reach the small intestine through the gastric acid in mice, it had potential to be biomacromolecular carrier of oral drug. Conclusion Proteins or peptides is easy to release in alkaline condition,but release few in acidic condition of pH2 (PH of gastric acid).The silica nanoparticles prepared have the potential to be oral drug carrier.

Analysis on the application of automatic oral drug dispensing system in our hospital / 国际中医中药杂志

The system construction and work flow of automatic oral drug dispensing system(AODDS) in our hospital are introduced,its' advantages and disadvantages of the application are analyzed.After applying AODDS,drug dispensing speed and accuracy are significantly increased.AODDS is conducive to promote hospital pharmaceutical care and pharmacy quality administration.The application of AODDS in our hospital may be referred for other hospitals to select AODDS.

Medicated chewing gum: a novel drug delivery system.

In the recent years scientific and technological advancements have been made in the research and development of oral drug delivery systems. The reasons that the oral route achieved such popularity may be primarily due to its ease of administration. Chewing gum is one of the very popular oral confectionary products. It is a potentially useful means of administering drugs either locally or systematically via, the oral cavity. The medicated chewing gum has through the recent years gained increasing acceptance as a drug delivery system. Chewing gum known as gum base (insoluble gum base resin) contains elastomers, emulsifiers, fillers, waxes, antioxidants, softners, sweeteners, food colorings, flavoring agents, and in case of medical chewing gum, active substances. It offers various advantages over conventional drug delivery systems. Unlike chewable tablets, medicated chewing gums are not supposed to be swallowed and may be removed from the site of application without resorting to invasive means. Moreover medicated chewing gums require the active and continuous masticatory activities for activation and continuation of drug release. An In-vitro apparatus was specially designed and constructed for release testing of medicated chewing gums. Medicated chewing gums are excellent mobile drug delivery systems for self-medication as it is convenient and can be administered discretely without water.

Automatic Oral Drug Dispensing System in Hospital Pharmacy:Application and Experience / 中国药房

OBJECTIVE: To provide references for the application of automatic oral drug dispensing system in hospital pharmacy. METHODS: The chief structure of automatic oral drug dispensing system in our hospital (TR-200FDS system) was introduced; the main working process and employment of this system were briefly introduced,and its advantages and disadvantages were discussed. RESULTS: The application of automatic oral drug dispensing system is characterized by convenience,cleanness,quickness and accuracy,but the relative costs are on the high side. CONCLUSION: The application of automatic oral drug dispensing system in hospital pharmacy can enhance hospital pharmaceutical care level,and it may represent the trend of the development in hospital pharmacy.

Application of Chitosan and it's Derivatives on Oral Drug Preparation / 中国海洋药物

Chitosan and it's derivatives have good biologic and particular physical and chemical properties. They have a wide applied foreground on drug preparations. This study introduced the recent advances of them based on widely researching the information and the actual works, and provided reference for the study of oral drug preparations.

Automatic Oral Drug Dispensing System Conducive to Hospital Pharmaceutical Care / 中国药房

OBJECTIVE:To realize automatic central drug dispensing model in hospital pharmacy.METHODS:The construction,running condition,major function and flow-sheet of automatic oral drug dispensing system of our hospital was introduced,and the automatic drug dispensing system was compared with traditional dispensing system.RESULTS:The automatic oral drug dispensing system could enhance the speed and accuracy of drug dispensing,shorten waiting time of nurse,improve health condition and decrease medicine pollution.CONCLUSION:The automatic oral drug dispensing system is suitable for drug dispensing in hospitals and conducive to the enhancing of pharmaceutical care level.