Ever-Increasing Role of Computational Tools in Solid-State Pharmaceutics: Advancing Drug Development with Enhanced Molecular Understanding and Risk Assessment.

The field of solid-state pharmaceutics comprises a broad range of investigations into various structural aspects of pharmaceutical solids, establishing a rational structure-property correlation. These solid systems allow the tunability of the physicochemical properties, such as solubility and dissolution, which in turn influence the pharmacokinetic and pharmacodynamic parameters of the active pharmaceutical ingredient (API). Hence, the study of physical characteristics of an API, e.

Quality-by-Design-Assisted Laboratory Scale-Up of Lipid Nanoparticles of Stearic Acid-Raloxifene Hydrochloride Conjugate: A Pathway for Enhanced Oral Bioavailability via Lymphatic Uptake.

Despite exhibiting promising efficacy in managing postmenopausal osteoporosis, hormonal therapy, and breast cancer prevention, the usage of raloxifene hydrochloride (RLX) is limited in clinical settings due to its low aqueous solubility (345.2 ± 15.6 μg/mL) and 2% oral bioavailability.

Navigating the brain: Harnessing endogenous cellular hitchhiking for targeting neoplastic and neuroinflammatory diseases.

Cellular hitchhiking is an emerging therapeutic strategy that uses an endogenous cell migration mechanism to deliver therapeutics to specific sites in the body. Owing to the low permeability and presence of the blood-brain barrier (BBB), the targeted delivery of therapeutics is limited, leading to inadequate localization in the brain. NCs fail to extravasate significantly into the tumor microenvironment (TME), demonstrating poor accumulation and tumor penetration.

Combating breast cancer-associated metastasis using paclitaxel and tranilast-loaded human serum albumin nanoparticles.

Objective: The objective of the current study is to combat breast cancer-associated metastasis using paclitaxel (PTX) and tranilast (TRA)-loaded human serum albumin (HSA) nanoparticles.

Significance: This combinatorial therapy uses microtubule stabilizing agent PTX, along with TGFβ inhibitor TRA. TRA may offer an improved therapeutic effect in breast cancer by inhibiting cell proliferation and metastasis.

A Mixed-Method Study of Exploring the Impact of Male Alcohol Dependence on Sexual Functioning and Marital Relationships.

Male alcohol dependence often leads to sexual dysfunction and disrupted marital relationships. This study aims to assess prevalence and pattern of sexual dysfunction amongst married male patients with alcohol dependence and influence of alcohol on their lives by exploring wives' perceptions. 100 married male patients with alcohol dependence and their wives ( = 70) were included.

Next-Generation Transformable Nanomedicines: Revolutionizing Cancer Drug Delivery and Theranostics.

Nanomedicine has significantly advanced the treatment of various cancer phenotypes, addressing numerous challenges associated with conventional therapies. Researchers have extensively investigated the physicochemical properties of nanocarriers, such as charge, morphology, and surface chemistry, to optimize drug delivery systems. In the context of transformable nanomedicine, these properties are particularly critical for overcoming existing limitations, including suboptimal blood circulation times, sequestration by the reticuloendothelial system and mononuclear phagocyte system, and inefficient targeting of the tumor microenvironment (TME).

Despicable role of epithelial-mesenchymal transition in breast cancer metastasis: Exhibiting restorative regimens.

Breast cancer (BC) is the most prevalent cancer in women globally. Anti-cancer advancements have enabled the killing of BC cells through various therapies; however, cancer relapse is still a major limitation and decreases patient survival and quality of life. Epithelial-to-mesenchymal transition (EMT) is responsible for tumor relapse in several cancers.

Docetaxel and niclosamide-loaded nanofiber systems for improved chemo-therapeutic activity and resistance reversal in prostate cancer.

Objective: The objective of the study was to tackle the recurrence of prostate cancer (PCa) post-surgery and to re-sensitize the docetaxel (DTX)-resistant PC-3 cells to chemo-therapy using NIC.

Significance: Prolonged DTX therapy leads to the emergence of chemo-resistance by overexpression of PI3K-AKT pathway in PCa along with tumor recurrence post-surgery. Suppression of this pathway could be essential in improving the anticancer activity of DTX and re-sensitizing the resistant cells.

Nanoparticle-enhanced delivery of resveratrol for targeted therapy of glioblastoma: Modulating the Akt/GSK-3β/NF-kB pathway in C6 glioma cells.

Objective: The study aims to explore Resveratrol (RES) as a potential therapeutic agent for Glioblastoma multiforme (GBM), a challenging brain cancer. RES, a polyphenolic compound with known benefits in various diseases including cancer, has shown promise in inhibiting glioma progression through its effects on the AKT signaling pathways. However, its limited ability to cross the blood-brain barrier restricts its clinical application in GBM treatment.

Three Strikingly Different Crystal Habits of Tadalafil: Design, Characterization, Pharmaceutical Performance, and Computational Studies.

The present study aims at improving the physicochemical properties of a widely used drug Tadalafil through crystal habit modification, without changing the polymorphic form. Three distinct types of crystal habits, namely, needle, plate, and block, were obtained under controlled crystallization protocols with optimized solvent compositions. Complete characterization of these three crystal habits was carried out using powder X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, and Fourier transform infrared spectroscopy.

Coamorphous systems of rebamipide: Selection of amino acid coformers based on protein-ligand docking, in vitro assessment and study of interactions by computational and multivariate analysis.

Three coamorphous systems of Rebamipide (REB) with the amino acids namely, Tryptophan (TRP), Phenylalanine (PHE) and Arginine (ARG) are reported. A unique approach for the virtual screening of amino acid coformers is presented by employing molecular docking studies based on interactions of the drug molecule with various amino acid fragments in the drug-receptor cocrystal structure. Successful formation of stable coamorphous systems with ARG, TRP and PHE served as the proof-of-concept along with negative benchmarking standards Histidine and Aspartic acid, wherein coamorphous systems could not be obtained despite multiple trials which resulted in crystalline physical mixtures.

Medications Affecting Outcomes and Prognosis of Dental Treatment: Part 1.

This article gives valuable insight into the effect of selected groups of medications on dental treatment outcome and prognosis. The review emphasizes the importance of thorough medical history, which may have an impact on the prognosis of dental treatment. We discuss drugs acting on the central nervous system, gastrointestinal tract, respiratory tract, endocrine system, and bone metabolism among others.

Unravelling the role of tumor microenvironment responsive nanobiomaterials in spatiotemporal controlled drug delivery for lung cancer therapy.

Design and development of efficient drug delivery technologies that impart site-specificity is the need of the hour for the effective treatment of lung cancer. The emergence of materials science and nanotechnology partially helped drug delivery scientists to achieve this objective. Various stimuli-responsive materials that undergo degradation at the pathological tumor microenvironment (TME) have been developed and explored for drug delivery applications using nanotechnological approaches.

Amelioration of breast cancer therapies through normalization of tumor vessels and microenvironment: paradigm shift to improve drug perfusion and nanocarrier permeation.

Breast cancer (BC) is the most commonly diagnosed cancer among women. Chemo-, immune- and photothermal therapies are employed to manage BC. However, the tumor microenvironment (TME) prevents free drugs and nanocarriers (NCs) from entering the tumor premises.

Exploration of Abiraterone acetate loaded Nanostructured lipid carriers for bioavailability improvement and circumvention of fast-fed variability.

Abiraterone acetate (ABA), a biopharmaceutical class IV drug suffers from solubility and permeability pitfalls resulting in limited oral bioavailability and positive food effect, i.e. multi-fold enhancement in drug absorption in the presence of food.

Quality by design empowered preparation of itraconazole albumin nanoparticles for prostate cancer.

The current advent explores the potential of itraconazole (ITR) in prostate cancer (PCa), by its incorporation into albumin nanoparticles (NP). ITR as a repurposed moiety has displayed tremendous potential in various cancers. However, poor aqueous solubility poses hurdles towards its clinical translation.

Surface Functionalized Lipid Nanoparticles in Promoting Therapeutic Outcomes: An Insight View of the Dynamic Drug Delivery System.

Compared to the conventional approach, nanoparticles (NPs) facilitate a non-hazardous, non-toxic, non-interactive, and biocompatible system, rendering them incredibly promising for improving drug delivery to target cells. When that comes to accomplishing specific therapeutic agents like drugs, peptides, nucleotides, , lipidic nanoparticulate systems have emerged as even more robust. They have asserted impressive ability in bypassing physiological and cellular barriers, evading lysosomal capture and the proton sponge effect, optimizing bioavailability, and compliance, lowering doses, and boosting therapeutic efficacy.

Quality by design fostered fabrication of cabazitaxel loaded pH-responsive Improved nanotherapeutics against prostate cancer.

Cabazitaxel has been approved for the treatment of prostate cancer since 2010. However, its poor solubility and permeability pitfalls prevent its accumulation at the target site and promote severe adverse effects. About 90% of prostate cancer (PCa) patients suffer from bone metastasis.

Supramolecular self-assembled peptide-engineered nanofibers: A propitious proposition for cancer therapy.

Cancer is a devastating disease that causes a substantial number of deaths worldwide. Current therapeutic interventions for cancer include chemotherapy, radiation therapy, or surgery. These conventional therapeutic approaches are associated with disadvantages such as multidrug resistance, destruction of healthy tissues, and tissue toxicity.

Quality by design endorsed atorvastatin-loaded nanostructured lipid carriers embedded in pH-responsive gel for melanoma.

Aim: Our aim was to repurpose atorvastatin for melanoma by encapsulating in a nanostructured lipid carrier matrix to promote tumour cell internalisation and skin permeation. pH-responsive chitosan gel was employed to restrict At-NLCs in upper dermal layers.

Methods: We utilised a quality by design approach for encapsulating At within the NLC matrix.

Sulfo-butyl ether β-cyclodextrin inclusion complexes of bosutinib: in silico, in vitro and in vivo evaluation in attenuating the fast-fed variability.

Bosutinib (BOS) is a BCS class IV drug that shows low oral bioavailability and high fast-fed variability. Various pharmaceutical formulations have been explored thus far in order to improve its bioavailability while avoiding fast-fed variability. In the present study, we explored cyclodextrin (CD) complexation strategy to overcome the aforementioned disadvantages associated with BOS.

Neutrophil membrane-based nanotherapeutics: Propitious paradigm shift in the management of cancer.

Cancer is the leading cause of death across the globe, with 19.3 million new cancer cases and 10 million deaths in the year 2020. Conventional treatment modalities have numerous pitfalls, such as off-site cytotoxicity and poor bioavailability.

Multifaceted roles of pollen in the management of cancer.

Oral drug delivery of microparticles demonstrates shortcomings like aggregation, decreased loading capacity and batch-to-batch variation, which limits its scale-up. Later, porous structures gained attention because of their large surface-to-volume ratio, high loading capacity and ability to carry biomacromolecules, which undergo degradation in GIT. But there are pitfalls like non-uniform particle size distribution, the impact of porogen properties, and harsh chemicals.

Quality by design endorsed fabrication of Ibrutinib-loaded human serum albumin nanoparticles for the management of leukemia.

Ibrutinib (IB), a BCS class II drug suffers from limited aqueous solubility, short half-life and extensive first-pass metabolism. In this project, we aim to recruit the desirable properties of human serum albumin (HSA) as a biocompatible drug carrier to circumvent nanoparticle-associated drawbacks. Quality by design and multivariate analysis was used for the optimization of IB-NPs.