Al Mustansiriyah Journal of Pharmaceutical Sciences

Fluocinolone acetonide (FA), a corticosteroid, was commonly used for treating inflammatory conditions but faced challenges due to poor water solubility, leading to low bioavailability and limited efficacy. To overcome these issues, FA was formulated as a nanosuspension (NS) within a hydrogel matrix. Nanosuspensions formulations were prepared using the precipitation method under ultra-sonication. The findings demonstrate that the prepared fluocinolone acetonide formulations' particle size values fell within the nanosized range. Carbopol at different concentrations (1%,1.5%,2%) was used as a gelling agent. The hydrogel formulations were evaluated through various characterization techniques, including skin irritation tests, spreadability, viscosity, in vitro release studies, ex vivo skin permeation studies, drug release kinetics, and compatibility studies. The results showed that Carbopol was safe, non-irritant, homogeneous, and provided high consistency with excellent spreadability. In vitro release studies demonstrated that FA release from the 1% Carbopol formula (FD1) was faster than that from 1.5% (FD2) and 2% (FD3) formulations. The Higuchi model best describes the drug release kinetics.

Ex vivo permeation studies revealed significantly higher permeation of FANS hydrogel compared to the pure drug hydrogel. FTIR spectra confirmed no significant interaction between the drug and gel base. In conclusion, FA was successfully formulated as a nanosuspension, and Carbopol effectively prolonged skin contact time, enhancing FA ,s therapeutic potential for topical administration.

Gastroretentive drug delivery systems (GRDDSs) are highly promising methods for the enhancement of the bioavailability and therapeutic effectiveness of some orally administered medications. The present review focused on gastroretentive film drug delivery methods, specifically developed to extend the duration of medication presence in the stomach which is most likely to enhance their absorption and efficacy.

The review examines different types of gastroretentive films, such as floating, mucoadhesive, and expandable films, emphasizing their respective modes of action, benefits, and drawbacks. Furthermore, the review includes an evaluation of gastroretentive films, which include in vitro buoyancy, swelling index, tensile strength, and drug release kinetics. The prospective clinical uses of these systems in the management of gastrointestinal problems and other medical conditions are also investigated. Lastly, the paper examines the difficulties and potential opportunities for the advancement and commercialization of gastro-retentive film drug delivery systems.

Gastroretentive drug delivery systems (GRDDSs) are highly promising methods for the enhancement of the bioavailability and therapeutic effectiveness of some orally administered medications. The present review focused on gastroretentive film drug delivery methods, specifically developed to extend the duration of medication presence in the stomach which is most likely to enhance their absorption and efficacy.

HCl release by evaluating key formulation and process parameters. The complexation technique was used to prepare PEC by adjusting Chitosan molecular weight and cross-linker concentration (1% and 2%). Formulations were assessed for drug content, buoyancy, raft strength, and in vitro drug release. Analytical methods such as FTIR, DSC, and FE-SEM confirmed PEC formation and structural properties. Drug release kinetics were modeled using mathematical equations. The finding demonstrates that increased Chitosan molecular weight and cross-linker concentration improved raft stability, buoyancy, and drug release control. The optimal formulation (F6) showed high drug content (94.8%), drug loading (11.9%), and sustained drug release over 12 hours. In conclusion, the optimized PEC raft system effectively prolonged Ond. HCl release offers a promising platform for drugs requiring extended gastric retention and controlled release.

In contemporary pharmaceutical design, controlled and sustained drug delivery has become the standard, leading to extensive research to improve drug product effectiveness, reliability, and safety. In situ gelling systems are polymeric formulations that initially exist as sol forms before being administered in the body but transition to gel forms under physiological conditions.

The benefits of in situ-forming polymeric delivery systems, such as ease of administration, reduced frequency of administration, and enhanced patient compliance and comfort, have generated this interest. Elements like temperature variation, pH alteration, ion presence, and ultraviolet irradiation influence the production of gels, this drug delivery system includes these features that enable its extensive application in the production of sustained delivery vehicles for bioactive compounds. Several biodegradable polymers, such as poloxamer, gellan gum, hydroxypropyl methylcellulose (HPMC), carboxymethylcellulose (CMC), pectin, chitosan, xanthan gum, and carbapol, are utilized in the development of in situ gels. From a manufacturing perspective, the production of such devices is less complicated, thereby reducing both investment and manufacturing costs. This review provides an overview of in situ gelling drug delivery systems, explores various approaches for these systems, discusses different types of polymers utilized, examines their evaluation and applications, and outlines some marketed products.

Patients with diabetes often experience a variety of electrolyte imbalances. These patients have significant disorders deficiencies in phosphate, magnesium, and potassium Both hypo- and hyper-natremia are associated with diabetes mellitus, which is indicative of the coexistence of processes related to hyperglycemia that tend to alter blood sodium in opposite ways.

Hyper tonicity, insulin insufficiency, potassium-sparing medications, and impaired renal function are other factors that contribute to the development of hyperkalemia. The electrolyte abnormalities that occur in diabetes mellitus are summarized in this article along with the fundamental mechanism. These strategiesare designed to realization should open the door to pathophysiology directed treatment, which will help prevent the various negative consequences linked to electrolyte imbalances and their management. In people with diabetes, electrolyte imbalances are frequent and may be linked to higher rates of morbidity and death. Those with decompensated diabetes mellitus, the elderly, and those with renal impairment are more likely to have these disruptions. Doctors prescribe complex treatment regimens that work to regulate electrolyte imbalance in diabetics in order to control blood sugar levels. It is best to understand the physiological mechanism of patients suffering from electrolyte imbalance, which plays an important role in controlling sugar levels in diabetics.

Transdermal delivery is recognized as one of
the most advantageous non-invasive drug
delivery technologies; but the skin's natural
barrier, particularly the stratum corneum,
restricts drug permeation. However,
ethosomes, which are phospholipid vesicles
containing ethanol, have the potential to
enhance transdermal drug delivery.
They are integrated into various vehicles to create innovative pharmaceutical formulations like
ethosomal gels (EGs). This study aimed to assess the appropriateness of various grades of carbopol
and hydroxypropyl methylcellulose (HPMC) as gel matrices for ethosomal suspensions intended
for transdermal delivery of loxoprofen (used as a model medication). Additionally, the effect of
lyophilization on hydrogel was studied. Five EGs (EG1-EG5) were developed and analyzed for
their viscosity, pH, drug content, and in vitro drug release. Additionally, the ex vivo penetration
of EG was compared with that in a gel formed from a hydroethanolic solution of drug (Sol-G).
The results revealed that, compared to HPMC, carbopol exhibited superior gelling properties, and
the drug release from the lyophilized optimized EG (EG5) was much higher (95.44±0.8%) over
12 hours than that of other formulations (p < 0.05). Moreover, the skin permeation investigation
employing rat skin indicated that the EG5 exhibited a markedly greater flux (J) value and apparent
permeability (Papp) in comparison to Sol-G. It can be concluded that the loxoprofen-loaded
ethosomes were successfully formulated in gel form and can be of use for transdermal delivery.

In recent years, great attention has been attentive to lipid-based drug delivery systems to concur with limitations associated with conventional formulations. Among these are solid lipid nanoparticles (SLNs) which are considered a promising delivery system because of the ease of manufacturing processes and scale-up proficiency, biocompatibility,

the biodegradability of ingredients involved in the formulation, and numerous additional advantages related to various routes of administration.

The present review provides insight into how SLNs are finding a role as promising nanocarriers and forms a comprehensive basis for overcoming problems related to traditional drug delivery systems. It also demonstrates variables affecting formulation, methods of preparation and evaluation, as well as routes of administration.

One of the significant adverse effects of statin medication is simvastatin-induced myopathy, for which there are few effective preventative measures. Simvastatin-induced skeletal muscle myopathy in male rats was assessed in this study utilizing immunohistochemical analysis of BAX (BCL2-associated protein X) expression to determine the preventive effects of Coenzyme Q10, Vitamin E, and their combination.

After being divided into groups, the rats were given simvastatin, Coenzyme Q10, vitamin E, or all three together for 30 days. The treatment groups' levels of BAX expression, a marker of apoptosis, were considerably lower than those of the group taking simvastatin alone. The biggest reduction was seen with the combination treatment, with an average immunohistochemistry (IHC) -intensity score of 1.0 ± 0.577, whereas the induction group's score was 2.857 ± 0.378. These results demonstrated the ability of vitamin E and Coenzyme Q10, particularly when combined, to reduce statin-induced muscle apoptosis. Future suggested treatment approaches to stop myopathy in statin users are based on the findings.

Heterocyclic compounds serve as crucial structural elements in the field of pharmaceutical medicinal chemistry. The five-membered heterocyclic nucleus of 1,3,4-oxadiazole occupies a distinctive position within medicinal chemistry and plays a vital role in the development of anticancer agents.
Recognized as a significant pharmacophore for approximately 85 years, 1,3,4-oxadiazole is in high demand across various biological and chemical disciplines. This small and straightforward nucleus is found in numerous compounds that are the focus of research concerning their properties, synthesis, derivatives, and pharmacological activities, including anticancer, antibacterial, antimalarial, anti-inflammatory, antidepressant, analgesic, and antiviral effects. The information regarding these activities presented in this article may prove beneficial to researchers, facilitating the discovery of new therapeutic agents for the benefit of society.

The percentage of microbial resistance to antibiotics has been remarkably increasing in the last decades. For this reason, there has been an increasing demand for using natural products molecules for medicinal purposes. The current study revealed the antimicrobial activity of aluminium potassium sulfate (alum) against the selected pathogens which includes gram positive and negative bacteria and fungus.Alum inhibits the growth of Pseudomonas aeruginosa and Staphylococcus aureus at all concentrations (50,40,30,20, 10 and 5 %).

The percentage of microbial resistance to antibiotics has been remarkably increasing in the last decades. For this reason, there has been an increasing demand for using natural products molecules for medicinal purposes. The current study revealed the antimicrobial activity of aluminium potassium sulfate (alum) against the selected pathogens which includes gram positive and negative bacteria and fungus.Alum inhibits the growth of Pseudomonas aeruginosa and Staphylococcus aureus at all concentrations (50,40,30,20, 10 and 5 %). However, Vibrio cholera growth was inhibited at the concentrations of (50, 40, 30, 20 and 10 %). The antimicrobial activity of alum against the selected pathogenic fungi (Cryptococcus neoformance , Cryptococcus gattii, Rhizopus micrococcus and Mucor circinelloiles) was measured. The results showed that alum has excellent antimicrobial activity against all the selected pathogenic fungi in all concentrations. With no inhibitory effect against both Rhizopus micrococcus and Mucor circinelloides at the lowest concentration of alum (5%). The growth of fungi is significantly reduced by 4-fold in the presence of alum in comparison with those grown in YPD media alone. Which means that half of antimicrobial activity of alum is due to inhibitory mechanism differ from the acidification. The above results confirmed the antimicrobial activity of alum against the selected pathogens, and proved that the inhibitory activity of alum is not only due to the low pH produced by alum but also to the presence of other inhibitory mechanism of alum. Regarding these results further study is needed to understand the inhibitory mechanisms of alum with neglecting the acidity effect of alum.

Formulating drugs for pediatric patients is more complex than for adults due to the diversity within this group. Solubility of active pharmaceutical ingredients (APIs) presents specific challenges, since children have unique physiological traits—smaller stomach volume and immature digestive systems—that affect absorption, metabolism, and overall drug effectiveness.

‏Oral formulations must consider drug sensitivity, swallowing difficulties, and compliance. Taste, ease of administration, and patient acceptance strongly influence therapeutic outcomes and safety. Ensuring children take medication as directed is often as important as the formulation itself.

‏To address these issues, solubility enhancement technologies have advanced

Tumor cells evolve adaptive mechanisms to function optimally within an acidic microenvironment. This adaptation is driven by the enhanced metabolic activity of tumors, which frequently results in acidosis and hypoxia. Carbonic anhydrase enzymes orchestrate cell homeostasis and affect cancer cell fate. Advances in structure-based design have enabled the identification of selective carbonic anhydrase XII inhibitors.

The study aimed to evaluate the anti-proliferative activity of sulfonamide derivatives and elucidate the plausible mode of action. MTT assay was conducted to evaluate cytotoxicity of acetazolamide, parent C3 and its derivatives C4 and C6 against breast cancer cell lines MCF-7, MDA-MB-231 and prostate cancer cells PC3. Further studies for C3, C4 and C6 compounds were conducted against MCF-7. Enzyme-linked immunosorbent assay of carbonic anhydrases IX and XII and fluorescent intracellular pH assay were conducted. Investigated compounds and acetazolamide reduced proliferation of all tested cells after 72 h. C3, C4, and C6 compounds reduced carbonic anhydrase XII concentrations. C3 and C6 did not appear significant reduction in CAIX in MCF-7. Conversely, C4 displayed statistically significant increase. Cells exposed to C3, C4, and C6 revealed a decrease in intracellular pH levels. In conclusion, all three compounds exhibited antiproliferative activities characterized by modulation of tumor pHi/pHe.

Background: To aid in the identification of drug candidates and the prediction of protein-ligand interactions, molecular docking predicts how ligands interact with receptors, aiding drug discovery. EGFR’s role in NSCLC makes quinazoline derivatives promising anticancer agents. However, accurately predicting their EGFR binding affinities remains a challenge.

Objectives: This research was designed to comparatively analyze three popular molecular docking tools; GOLD, Glide, and MOE by comparing their performance in predicting quinazoline derivative binding poses and affinities against EGFR. This study aimed to identify the most effective docking tool for screening quinazoline-based antiproliferative drugs.

Method: Quinazoline derivatives were docked into the EGFR receptor binding site using GOLD, Glide, and MOE. The ligands were energy-minimized, and the proteins were prepared by removing water molecules and adding hydrogen atoms. Docking simulations ran under default settings, comparing binding affinities via various scoring functions.

Results: GOLD identified N-(CH3)3 and 3-NO₂ derivatives as strong binders, while Glide favored Erlotinib due to π-π stacking interactions. MOE highlighted Ethyl Vanillin and N-(CH3)3 derivatives, particularly for their polar interactions. The docking results demonstrated that each program had strengths depending on the ligand's interaction type.

Conclusion: GOLD and MOE showed the most promise in identifying high-affinity binders for quinazoline derivatives targeting EGFR, while Glide excelled in handling hydrophobic interactions. The findings highlight the importance of selecting the appropriate docking tool based on ligand characteristics to optimize the drug discovery process for EGFR inhibitors.

The targeted delivery of chemotherapy drugs to their specific locations in a tumor is a cornerstone of current oncology for high therapeutic efficacy and reduced systemic toxicity. Recent breakthroughs in nanotechnology, molecular and imaging modalities have revolutionized the field of targeted delivery and tracking technology. With these new advances, the real-time tracking of drug routes and increased accuracy in tumor localization have become a reality.

This review has discussed advanced targeting approaches, such as passive and active targeting, multifunctional theranostics and stimuli-responsive platforms to describe their mechanism, clinical utility and challenges. In addition, tracking modalities such as magnetic resonance imaging (MRI) and positron emission tomography (PET) have played a key role in noninvasive tracking and have been discussed in detail. Challenges such as immune clearance, tumor heterogeneity and translational barriers have been discussed, and new avenues through artificial intelligence, biomarker-guided approaches and therapeutic platforms have been explored in detail. Emerging studies have also shed new light on targeted oncology, combining biomarker discovery and new therapeutic platforms with individualized patient requirements. A thorough analysis reveals an interdisciplinary obstacle in developing targeted delivery technology and shaping future cancer therapy.

Hyaluronic acid, also known as hyaluronan, is a hydrophilic, negatively charged extracellular matrix ofglycosaminoglycan polymer with liable to change molecular weight that control its physiological role, rheological properties and uses. The main goal is to measure the effectiveness and the range of side effects of two different forms of hyaluronic acid, in patients with knee osteoarthritis. in this particular controlled, randomized, collateral group study, 30 patients , which are confirm to be suffering of knee OA with an intense pain discomfort ,all were assigned randomly to receive one of the two formulation of HA under the study cross- linked hylornic acid + mannitol and natural hyaluronan. Symptoms and function parameters were assessed after injection . At the terminal stage of the treatment, both of the candidates and specialist general evaluations were taken into consideration.In this study, we note that the two injections of HA have a clear effect on pain ,stiffness and physical function of patients after injecting HA, yet once comparing the both of HA ,it was noticeable that no difference in their effect on patients, meaning that both injections of HA are effective, but the relative difference between them is the cost and also the number of doses in the course , as the Monvisc injection, the cost of one injection is 330k IQD, and 3 doses must be taken in the course, i.e. the total is 990k IQD, while Arthromac needs single injection, and the cost is 240k IQD. As a Conclusion it was concluded that the effectiveness of IA injections of HMW-HA in various formulations is about similar, while some may be chosen over others depending on the brand, the treating physician, the price, and the total number of injections. Regarding safety, hyaluronic acid is generally considered to be safe.

The vast advancement in pharmaceutical analysis technology, and the evolutionary rise in molecular Biology following the milestone coding of the human genome and the splendid utilisation of computational chemistry and bioinformatics, have called for urgent employment of knowledge, tools and skills to optimise therapies and clinical management. Oral iron chelators have long been in the market but nevertheless require a quality booster to parallel the overall upgrade in all life aspects let alone clinical advances, drugs, and therapeutics.

The implementation for such development lies in the hands of medicinal chemists and experts in drug design and discovery. Using bioinformatic approaches, this study aims to predict an ideal structural configuration capable of producing a more effective compound than the long-used oral iron chelator, Deferiprone.

In pursuit of such an aspiration, a range of fluorinated hydroxypyridinones (the backbone structure for Deferiprone) have been investigated. Fluorination of drugs in general, has recently been shown to bring about many desired features such as metabolic stability. ADMET lab 2.0 along with few other software that are used in molecular docking; have been brought into play to unfold an ideal, more potent fluorinated hydroxypyridinone than Deferiprone particularly with regards to the toxicity profile.