Recent advances in drug delivery and formulation最新文献

Background: The Cataract is the leading cause of visual impairment and preventable blindness worldwide. Cataract removal surgery involves various post-operative complications like pain and inflammation.

Objectives: The objective of this study is to screen the polymer concentration as well as optimize the formulation components to develop the pluronic micelles with nanosized characterization and for enhanced corneal permeation study.

Methodology: For optimization, Central Composite design was employed to study the effect of independent variables, concentration of Pluronic F 127 (X1) and the concentration of Hyaluronic acid (X2) on chosen responses (Y 1 ) Micelle size, (Y 2 ) Entrapment Efficiency, (Y 3 ) Viscosity. The lyophilised powder was used for physical characterisation.

Results: The formulation containing 5%w/v Pluronic F127 and 0.2%w/v Hyaluronic acid was the optimised composition with micelle size and zeta potential 38.74±4.12nm and -17.6±0.1 mV respectively. In-vitro drug release was found to be 91.72±1.2 percentage in 8 hours. Surface morphology revealed micelles were spherical in shape. Ocular irritancy study showed that formulation was safe and non-irritant. In vitro corneal permeation studies through excised rabbit cornea indicated 1.5 fold increase in ocular availability without corneal damage compared to an aqueous suspension containing the same amount of drug in nanomicelles.

Conclusion: In a nutshell, Pluronic Nanomicelles would be a platform for the delivery of Bromfenac Sodium.

Background: The Hot Melt Extrusion (HME) technique has shown tremendous potential in transforming highly hydrophobic crystalline drug substances into amorphous solids without using solvents. This review explores in detail the general considerations involved in the process of HME, its applications and advances.

Objective: The present review examines the physicochemical properties of polymers pertinent to the HME process. Theoretical approaches for the screening of polymers are highlighted as a part of successful HME processed drug products. The critical quality attributes associated with the process of HME are also discussed in this review. HME plays a significant role in the dosage form design, and the same has been mentioned with suitable examples. The role of HME in developing several sustained release formulations, films, and implants is described along with the research carried out in a similar domain.

Methods: The method includes the collection of data from different search engines like PubMed, ScienceDirect, and SciFinder to get coverage of relevant literature for accumulating appropriate information regarding HME, its importance in pharmaceutical product development, and advanced applications.

Results: HME is known to have advanced pharmaceutical applications in the domains related to 3D printing, nanotechnology, and PAT technology. HME-based technologies explored using Design-of- Experiments also lead to the systematic development of pharmaceutical formulations.

Conclusion: HME remains an adaptable and differentiated technique for overall formulation development.

Coronavirus disease (COVID-19) emerged in China in December 2019. In March 2020, the WHO declared it a pandemic leading to worldwide lockdowns and travel restrictions. By May, it infected 4,789,205 and killed 318,789 people. This led to severe shortages in the medical sector besides devastating socio-economic effects. Many technologies such as artificial intelligence (AI), virtual reality (VR), microfluidics, 3D printing, and 3D scanning can step into contain the virus and hinder its extensive spread. This article aims to explore the potentials of 3D printing and microfluidic in accelerating the diagnosis and monitoring of the disease and fulfilling the shortages of personal protective equipment (PPE) and medical equipment. It highlights the main applications of 3D printers and microfluidics in providing PPE (masks, respirators, face shields, goggles, and isolation chambers/hoods), supportive care (respiratory equipment) and diagnostic supplies (sampling swabs & lab-on-chip) to ease the COVID-19 pressures. Also, the cost of such technology and regulation considerations are addressed. We conclude that 3D printing provided reusable and low-cost solutions to mitigate the shortages. However, safety, sterility, and compatibility with environmental protection standards need to be guaranteed through standardization and assessment by regulatory bodies. Finally, lessons learned from this pandemic can also help the world prepare for upcoming outbreaks.

Background: Drug laden implantable systems can provide drug release over several hours to years, which eventually aid in the therapy of both acute and chronic diseases. The present study focuses on a fundamental evaluation of the influence of implant properties such as morphology, architecture, porosity, surface area, and wettability in regulating the drug release kinetics from drug-loaded polymeric matrices.

Methods: For this, Polydioxanone (PDS) was selected as the polymer and Paclitaxel (Ptx) as the model drug. Two different forms of the matrix implants, viz., reservoir type capsules developed by dip coating and matrix type membranes fabricated by phase inversion and electrospinning, were utilized for the study. Drug release from all the four different matrices prepared by simple techniques was evaluated in vitro in PBS and ex vivo in peritoneal wash fluid for ~4 weeks. The drug release profiles were thereafter correlated with the physicochemical parameters of the polymeric implants.

Results: Reservoir-type capsules followed a slow and steady zero-order kinetics, while matrix-type electrospun and phase inversion membranes displayed typical biphasic kinetics.

Conclusion: It was inferred that the slow degradation rate of PDS polymer as well as the implant properties like porosity and wettability play an important role in controlling the drug release rates.

The term "reactive oxygen species" (ROS) refers to a family of extremely reactive molecules. They are crucial as secondary messengers in both physiological functioning and the development of cancer. Tumors have developed the ability to survive at elevated ROS levels with significantly higher H2O2 levels than normal tissues. Chemodynamic therapy is a novel approach to cancer treatment that generates highly toxic hydroxyl radicals via a Fenton/Fenton-like reaction between metals and peroxides. Inorganic nanoparticles cause cytotoxicity by releasing ROS. Inorganic nanoparticles can alter redox homoeostasis by generating ROS or diminishing scavenging mechanisms. Internalized nanoparticles generate ROS in biological systems independent of the route of internalisation. This method of producing ROS could be employed to kill cancer cells as a therapeutic strategy. ROS also play a role in regulating the development of normal stem cells, as excessive ROS disturb the stem cells' regular biological cycles. ROS treatment has a significant effect on normal cellular function. Mitochondrial ROS are at the centre of metabolic changes and control a variety of other cellular processes, which can lead to medication resistance in cancer patients. As a result, utilising ROS in therapeutic applications can be a double-edged sword that requires better understanding.

Vaccines are one of the greatest medical achievements of modern medicine. The nasal mucosa represents an effective route of vaccination for both mucosal immunity and peripheral, being at the same time an inductive and effector site of immunity. In this paper, the innovative and patented compositions and manufacturing procedures of nanomaterials have been studied using the peerreviewed research literature. Nanomaterials have several properties that make them unique as adjuvant for vaccines. Nanoadjuvants through the influence of antigen availability over time affect the immune response. Namely, the amount of antigen reaching the immune system or its release over prolonged periods of time can be effectively increased by nanoadjuvants. Mucosal vaccines are an interesting alternative for immunization of diseases in which pathogens access the body through these epithelia. Nanometric adjuvants are not only a viable approach to improve the efficacy of nasal vaccines but in most of the cases they represent the core of the intellectual property related to the innovative vaccine.

Cancer is a worldwide health ailment with no known boundaries in terms of mortality and occurrence rates, thus is one of the biggest threats to humankind. Hence, there is an absolute need to develop novel therapeutics to bridge the infirmities associated with chemotherapy and conventional surgical methodologies, including impairment of normal tissue, compromised drug efficiency and an escalation in side effects. In lieu of this, there has been a surge in curiosity towards the development of injectable hydrogels for cancer therapy because local administration of the active pharmaceutical agent offers encouraging advantages such as providing a higher effective dose at the target site, a prolonged retention time of drug, ease of administration, mitigation of dose in vivo, and improved patient compliance. Furthermore, due to their biocompatible nature, such systems can significantly reduce the side effects that occur on long-term exposure to chemotherapy. The present review details the most recent advancements in the in-situ gel forming polymers (natural and synthetic), polymeric cross-linking methodologies and in-situ gelling mechanisms, focusing on their clinical benefits in cancer therapy.

Background: Gold nanoparticles have the potential to be used as a carrier in drug delivery systems due to their small size, large surface area and short circulation time in blood.

Objective: This study demonstrates that doxorubicin conjugation with gold nanoparticles (AuNPs) may reduce its toxicity as well as improve therapeutic efficacy.

Methods: Five groups of Albino rats were used; 1: healthy control, 2: injured, 3: injured and treated with Dox, 4: injured and treated with AuNPs, 5: injured and treated with AuNPs: Dox. At the end of the experiment, blood and liver tissues were processed for biochemical and histopathological analysis. The expression of collagen, HO-1, IL-6 and TNF-α genes involved in liver fibrosis was observed through real-time PCR.

Results: At the end of the experiment, it was observed that the body weights of DOX-treated rats decreased by 0.72%, however, AuNPs and Au: DOX-treated rats were 15.3% and 29.13% respectively. The percentage of liver protection determined through alanine aminotransferase and aspartate aminotransferase levels in DOX, AuNPs and AuNPs: DOX treated groups were 39.21%, 79.26%, 98.17% and 47.77%, 84.17%, 97.92%, respectively, representing better recovering liver in Dox-AuNPs treated rats compared to others. Histopathological and gene expression studies further support the findings. The mRNA expression levels of inflammatory and oxidative stress-related genes HO-1, IL-6 and TNF- α were upregulated in the injured group but downregulated in the treated group.

Conclusion: As depicted through biochemical, histopathological and gene expression studies, Au: DOX conjugate group seems to be protective against liver fibrosis.

Background: The oral route is a highly recommended route for the delivery of a drug. But most lipophilic drugs are difficult to deliver via this route due to their low aqueous solubility. Selfemulsifying drug delivery systems (SEDDS) have emerged as a potential approach of increasing dissolution of a hydrophobic drug due to spontaneous dispersion in micron or nano sized globules in the GI tract under mild agitation.

Objective: The main motive of this review article is to describe the mechanisms, advantages, disadvantages, factors affecting, effects of excipients, possible mechanisms of enhancing bioavailability, and evaluation of self-emulsifying drug delivery systems.

Results: Self emulsifying systems incorporate the hydrophobic drug inside the oil globules, and a monolayer is formed by surfactants to provide the low interfacial tension, which leads to improvement in the dissolution rate of hydrophobic drugs. The globule size of self-emulsifying systems depends upon the type and ratio of excipients in which they are used. The ternary phase diagram is constructed to find out the range of concentration of excipients used. This review article also presents recent and updated patents on self-emulsifying drug delivery systems. Self-emulsifying systems have the ability to enhance the oral bioavailability and solubility of lipophilic drugs.

Conclusion: This technique offers further advantages such as bypassing the first pass metabolism via absorption of drugs through the lymphatic system, easy manufacturing, reducing enzymatic hydrolysis, inter and intra subject variability, and food effects.