: Acne vulgaris represents a chronic inflammation of the pilosebaceous apparatus, predominantly affecting the face and upper trunk due to the high concentration of sebaceous glands in these regions. Sulfanilamide is a sulfonamide antibacterial drug, a class of antibiotics that inhibit bacterial DNA synthesis by competitive antagonism of PABA. In this study, a novel patch formulation was developed for the effective treatment of acne using biocompatible polymers, hydroxypropyl methylcellulose (HPMC) and chitosan, as the matrix materials, and sulfanilamide as the active agent. The patches were prepared employing varying concentrations of chitosan (0.25%, 0.5%, and 1%), HPMC (0.125%, 0.25%, and 0.5%), and sulfanilamide (0.25%, 0.5%, and 0.75%) solutions. In this study, customized Design of Experiments (DoE) and response surface methodology (RSM) were applied to clarify the effect of the concentration of chitosan (X1), HPMC (X2), and sulfanilamide (X3) on swelling (Y1), porosity (Y2), and absorbency (Y3). Multi-response optimization analysis was conducted to identify the optimal formulation exhibiting maximum absorbency, minimum swelling, and appropriate porosity. The optimized patch formulation was subsequently characterized using Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), in vitro drug release studies, and antibacterial activity studies. The findings revealed that the optimized formulation achieved controlled drug release along with notable antibacterial efficacy. Therefore, a controlled-release transdermal patch was successfully formulated for the effective treatment of acne.

Objective: This study aims to formulate and optimize hydroxypropyl methylcellulose (HPMC)-based microparticles for the vaginal delivery of ibuprofen using a full factorial design approach, aiming for sustained drug release, enhanced local effect, and reduced systemic exposure.Material and Method: Ibuprofen-loaded HPMC microparticles were prepared via the simple desolvation method using dichloromethane (DCM) as solvent and liquid paraffin as the continuous phase. The HPMC:DCM ratio and volume of paraffin were selected as independent variables, while particle size and drug loading efficiency were evaluated as responses. Particle characterization was performed using Zetasizer, SEM, and DSC. In vitro drug release was assessed under simulated vaginal conditions (pH 4.5)Result and Discussion: Particle sizes ranged from 1.09 to 10.23 µm with polydispersity indices below 0.5, indicating acceptable uniformity. Drug loading efficiency was between 66.47% and 89.23%, increasing with higher HPMC concentrations. In vitro release studies demonstrated sustained ibuprofen release, reaching approximately 88% over 180 minutes. ANOVA confirmed that the HPMC:DCM ratio significantly affected both particle size and drug entrapment (p < 0.0001). The optimized HPMC-based microparticles provide a promising vaginal drug delivery system for ibuprofen, offering controlled release, high drug loading, and potential for improved therapeutic efficacy with reduced systemic side effects.

This study aimed to develop and evaluate semi-solid topical formulations containing oleuropein, a phenolic compound with strong antioxidant and anti-inflammatory activity, for wound and burn treatment. The primary hypothesis was that optimizing formulation type would improve oleuropein stability, release behavior, and dermal compatibility, thereby enhancing therapeutic performance. Oleuropein isolated from olive leaves was incorporated into ointment (F1), cream (F2), and gel (F3) formulations at 1%, 2.5%, and 5%. Physicochemical characterization included pH, rheology, drug content, and in vitro release. UV-Vis spectrophotometric analysis at 280 nm was optimized to prevent excipient interference and ensure selective quantification in semi-solid matrices. Drug release was evaluated using the dialysis bag method, and stability was assessed under short-, long-term, and accelerated conditions by monitoring active content and viscosity. Among all formulations, the cream F2.1 showed the most favorable profile, with a physiologically compatible pH (∼5.4) and high initial viscosity (64 Pa·s at 5 rpm, TF-96 spindle), exhibiting shear-dependent reduction consistent with non-Newtonian pseudoplastic flow suitable for dermal application. F2.1 achieved 13.5% cumulative release over 7 h, indicating modified delivery. Stability studies demonstrated acceptable active retention under standard conditions, while partial degradation occurred under accelerated storage. Overall, F2.1 provided improved stability and modified topical delivery, supporting further biological and in vivo evaluation.

Powder compaction remains the key step in pharmaceutical tablet manufacturing, but its multiscale and path-dependent nature makes accurate prediction of tablet properties difficult. Compression equations have long been used to relate applied pressure to densification, porosity, and mechanical strength, providing descriptors for material comparison and formulation design. Classical models such as Heckel, Kawakita-Lüdde, and Cooper-Eaton remain widely used, although they are limited by pressure-range dependence, sensitivity to in-die versus out-of-die measurements, and restricted mechanistic interpretation. Recent developments have expanded compression modeling to include extended in-die formulations incorporating solid compressibility, continuum constitutive laws for finite-element simulations, particle-scale discrete-element approaches, and data-driven process analytical technology (PAT) frameworks. These approaches are critically evaluated alongside classical equations with respect to constitutive validity, calibration transferability, contact-law realism, computational cost, data governance, model drift, and regulatory acceptability. Together, they form a hierarchical modeling framework spanning empirical screening, mechanistic prediction, and real-time process control. This review integrates classical and emerging compaction models and discusses their relevance to critical quality attributes, scale-up, and digital-twin-enabled pharmaceutical manufacturing.

Orally disintegrating tablets (ODTs) are solid oral dosage forms designed to disintegrate in the oral cavity within one minute without requiring water, offering significant advantages for elderly individuals, children, and patients with swallowing difficulties. The objective of this study was to formulate and evaluate fast disintegrating tablets containing ketoprofen using the direct compression method and to investigate the influence of different excipients on critical in vitro quality control parameters. Two tablet formulations were prepared, each containing 150 mg of ketoprofen as the active pharmaceutical ingredient. Excipients included croscarmellose sodium, sucrose-calcium phosphate co-processed filler, mannitol, microcrystalline cellulose, magnesium stearate, and talc. Tablets were evaluated for diameter, thickness, weight variation, hardness and in vitro disintegration time. Both formulations demonstrated acceptable physical properties, but the formulation containing microcrystalline cellulose and mannitol showed markedly faster in vitro disintegration time (40.5 ± 3.6 seconds) compared with the formulation prepared with sucrose-calcium phosphate (159.5 ± 18.6 seconds). The results indicate that mannitol is a more suitable filler than sucrose-calcium phosphate for fast disintegrating ketoprofen tablet systems and that 150 mg ketoprofen is an adequate dose for this dosage form.

Background and Aims: This study investigated the potential of naltrexone hydrochloride (NH) loaded water-in-oil (W/O) microemulsions (ME) as an alternative treatment strategy for cutaneous leishmaniasis caused by Leishmania tropica. This study aims to provide a topical alternative to the treatment of leishmaniasis, while also identifying a new therapeutic use of naltrexone other than its use in opioid addiction. Methods: Stable water-in-oil microemulsion formulations were developed using linseed oil, Span 60 (R), and polyethylene glycol 400. Microemulsions were prepared using triangle phase diagrams and optimization was performed by determining the droplet size, viscosity, pH, conductivity, and zeta potential values. The antileishmanial activity of the optimized microemulsion formulation was tested under in vitro conditions. Results: The optimized formulation (ME-2) demonstrated favorable physicochemical properties, including a droplet size of 99.86 nm, low polydispersity index (0.242), and high zeta potential (-42.9 mV), ensuring stability and homogeneity. In vitro release studies indicated first-order kinetics, suggesting the controlled release of NH. The antileishmanial activity of ME-2 was evaluated against L. tropica promastigote, revealing a 50% inhibition at an IC50 concentration of 5.17 mu M. While amphotericin B, the gold standard, exhibited superior efficacy (IC50 = 0.063 mu M), NH demonstrated a dose-dependent reduction in promastigote viability. This suggests its potential as a supplementary treatment, particularly in cases where amphotericin B's toxicity is a concern. Conclusion: Future studies focusing on structural optimization, mechanism elucidation, and in vivo validation could enhance NH's efficacy, offering a promising alternative for leishmaniasis management. This work establishes a foundational basis for leveraging NH microemulsions in parasitic disease therapy.

Amaç: Göz kuruluğunu önlemek için kullanılan göz damlalarının gözde kalış süresinin kısa olmasıyla alternatif dozaj şekillerinin araştırılmasını gerektirmiştir. İn-situ hidrojeller, saklama sırasında sol fazında olup çevresel koşullarda jel fazına geçerek hedef bölgede daha uzun süre kalabilmektedir. Bu çalışmada, doğal ve biyouyumu polimerler kullanılarak göz sıcaklığında sol-jel geçişi yapabilen in-situ hidrojel formülasyonları geliştirilmiş ve karakterizasyonları gerçekleştirilmiştir. Gereç ve Yöntem: HA, CMC, PAA ve sitrik asit, fiziksel karıştırma yöntemi esas alınarak 37°C sıcaklıkta distile su içerisine serpilerek homojen dağılımı sağlanmıştır. Göz fizyolojisine uygunluğu karakterizasyon çalışmaları ile kontrol edilmiştir. pH ölçümü, şişme/erozyon ve sol-jel geçiş sıcaklığı değerlendirilmesi ve viskozite ölçümü karakterizsyon çalışmaları altında gerçekleştirilmiştir. Tüm veriler değerlendirilerek optimum özelliklere sahip en uygun formülasyon/lar seçilerek hızlandırılmış stabilite çalışmaları gerçekleştirilmiştir. Sonuç ve Tartışma: Su tutma kapasitesi yüksek, biyouyumlu, gözde uzun süre kalabilen in-situ hidrojel formülasyonları için hyaluronik asit, poliakrilamid ve karboksimetil selüloz kombinasyonu uygun bulunmuştur. 7 günlük hızlandırılmış in vitro stabilite çalışmasında, formülasyonların pH ve viskozite değerlerinde önemli bir değişiklik gözlenmemiştir.

Ivermectin (IVM), a broad-spectrum antiparasitic agent that has been extensively used in both human and veterinary medicine for decades. Conventional formulations of IVM are challenged by poor aqueous solubility, low bioavailability, and limited tissue targeting, which can limit its therapeutic potential, despite its clinical success. The investigation of novel dosage forms and drug delivery technologies has been facilitated by recent advancements in pharmaceutical sciences, with the objective of improving the pharmacokinetic and pharmacodynamic profiles of IVM. Innovative systems, including lipid-based drug delivery systems, nanoparticles, polymeric carriers, solid lipid nanoparticles, and nanostructured lipid carriers, have demonstrated significant potential in terms of their ability to enhance solubility, facilitate controlled and targeted drug release, and reduce systemic toxicity. Additionally, these advanced systems open new possibilities for repurposing IVM in therapeutic areas beyond parasitic infections, including antiviral and anticancer applications. This review highlights the current progress and future prospects of modern dosage forms designed to optimize IVM delivery and broaden its clinical utility. Thereby providing an in-depth and critical evaluation of advanced IVM dosage forms, with a particular emphasis on their design rationale, pharmacokinetic enhancements, and capacity to address the limitations associated with conventional formulations.

Ivermectin (IVM), an antiparasitic drug approved by the Food and Drug Administration (FDA), is widely used to treat several neglected tropical diseases, including onchocerciasis, helminthiases, and scabies. Additionally, IVM has shown potential as a potent inhibitor of certain RNA viruses, such as SARS-CoV-2. However, IVM is highly hydrophobic, essentially insoluble in water, which limits its bioavailability and therapeutic effectiveness. The use of liposomes as drug carriers offers several advantages, including enhanced solubility for lipophilic drugs, passive targeting of immune system cells, sustained release, and improved tissue penetration. To address the limitations of IVM, including its poor solubility and bioavailability, liposomal formulations were developed using a combination of soyphosphatidylcholine (SPC), dioleylphosphatidylcholine (DOPC), cholesterol (Ch), and diethylphosphate (DCP) in two distinct molar ratios (1.85:1:0.15 and 7:2:1) via the ethanol injection method. The physicochemical properties of the placebo and IVM-loaded liposomes were extensively characterized in our earlier study, including the particle size, polydispersity index, and zeta potential. The present work adds a deeper level of investigation into how to effect cellular uptake and cytotoxicity in vitro of both free IVM and IVM-loaded liposomes in Vero E6 cells. The half-maximal cytotoxic concentrations (CC 50 ) for free IVM and IVM-loaded liposomes were 10 μM and > 110 μM, respectively and the cellular uptake of IVM-loaded liposomes ranged from 13 to 60%, whereas free IVM showed a significantly lower uptake of only 2%. These results demonstrate that liposomal encapsulation effectively enhances IVM’s cellular uptake while reducing its cytotoxicity, thus offering a promising strategy for improving the effectiveness of IVM. Graphical Abstract

Flap surgery is an integral part of plastic surgery, and ischemia-reperfusion (I/R) injury significantly affects the viability of the flap. Carvedilol (CRV), a nonselective beta-blocker with alpha-1 blocking and antioxidant properties, and known for its potential in reducing I/R damage, was chosen as the active substance for our study. The aim of this study was to investigate the vasodilator and antioxidant effects of CRV on rat inferior epigastric artery skin flap using orally disintegrating tablets (ODTs). The optimized ODT formulation was subjected to in vivo experiments using Sprague-Dawley female rats (n = 24) divided into three groups: Group I (control, I/R), Group II (treatment, I/R + CRV), and Group III (treatment, I/R), I/R + CRV ODT). Reperfusion was then observed following the release of the microclamp from the pedicle, and the flap was then re-adapted to its original position. Control rats were given oral isotonic solution via gavage and were subjected to 8 h of ischemia and 12 h of reperfusion. Group II was given 2 mg/kg CRV oral tablets for 7 days before and after surgery. Group III was given 2 mg/kg/day CRV ODT for the same period. Biopsies were taken from the flap and histopathological and biochemical analyses including superoxide dismutase, glutathionenitric oxide, malondialdehyde, paraoxonase 1, total oxidant, and total antioxidant capacities were performed. This study demonstrates that CRV ODTs significantly increased flap viability by approximately 25% compared to the control group, highlighting their promising therapeutic potential.

Objective: Mucoadhesive polymers have emerged as crucial components in the realm of drug delivery systems, particularly in the context of targeted treatments within the colon. These polymers possess adhesive properties that enable them to form temporary bonds with mucosal surfaces, extending the contact time of drugs with the colonic mucosa. This review provides a comprehensive overview of mucoadhesive polymers for colon drug delivery systems. Natural polymers such as chitosan and alginate, along with synthetic counterparts like polyacrylic acid derivatives, find application in these systems. The advantages of mucoadhesive polymers lie in their ability to facilitate site-specific drug delivery, thereby minimizing systemic side effects, and in enabling controlled and sustained release of drugs for improved bioavailability. Despite these benefits, challenges including variability in mucosal conditions and the imperative need for biocompatibility must be addressed. The applications of mucoadhesive polymers span diverse medical conditions, including targeted delivery of anti-inflammatory drugs for inflammatory bowel diseases, localized administration of chemotherapeutic agents for colon cancer treatment, and precise delivery of antibiotics for colonic infections. Result and Discussion: As a promising avenue for optimizing colon drug delivery, mucoadhesive polymers offer great potential for the development of effective and well-tolerated treatments for various colonic disorders.

The study aimed to evaluate in vitro and in vivo oral rapid mini tablets containing atomoxetine hydrochloride (ATO), developed for children with Attention Deficit and Hyperactivity (ADHD). An inclusion complex of ATO with β-cyclodextrin (β-CD) was prepared to mask the bitter taste of ATO and make it suitable for oral administration to children. ODMTs were administered to ADHD mice born from nicotine-administered mother mice during pregnancy and lactation, allowing the assessment of their efficacy in vivo setting. Results obtained from the open field test, new object recognition test, and Barnes maze test revealed that the ODMT formulation containing ATO-β-CD inclusion complexes exhibited potential as an alternative to the capsule form of ATO. As a conclusion, factorial experimental design was employed in the preparation of ATO-β-CD complexes and ODMTs, and the experimental animals were subjected to hyperactivity induced by nicotine, thereby providing a distinct context in which the developed ODMT formulation was evaluated.

Objective: This study aimed to create an orally disintegrating tablet (ODT) formulation using an itraconazole (ITZ)-beta-cyclodextrin (β-CD) complex to enhance itraconazole's solubility, a drug with limited solubility. β-CD was chosen for its compatibility with ITZ. Material and Method: The study prepared equimolar mixtures of ITZ and β-CD through kneading, assessing their solubility and dissolution rates. The inclusion complexes significantly increased ITZ's solubility. This complex was used to develop directly compressed ODTs with a lower ITZ content (25 mg), incorporating D-Mannitol as a bulking agent, sweetener, and to enhance mouthfeel, facilitating rapid disintegration and drug release. Result and Discussion: ODT formulations containing the ITZ-β-CD complex showed a significantly higher dissolution rate of ITZ compared to formulations with pure ITZ. This enhancement in dissolution is expected to significantly improve ITZ's bioavailability, suggesting a potential for reducing ITZ dosage and minimizing adverse effects.

Objective: Orally Disintegrating Tablets (ODTs) have revolutionized pharmaceutical drug delivery, offering a patient-friendly alternative for those struggling with conventional tablet swallowing. This study delves into the impact of superdisintegrants (crospovidone, sodium starch glycolate, and croscarmellose sodium) on the in vitro characterization of Ketoprofen-containing ODTs. ODTs are designed to rapidly disintegrate in the oral cavity without water, enhancing patient compliance, ensuring faster therapeutic onset, and providing convenience. Material and Method: The micromeritic properties of pre-compression Ketoprofen ODT blends were assessed for bulk density, tapped density, Hausner ratio, and compressibility index. ODTs were formulated using a direct compression method to maintain component uniformity. Comprehensive characterization included weight variation, tablet hardness, friability, wetting time, and in vitro disintegration time assessments. The drug content was determined through UV spectrophotometry of dissolved ODTs, and dissolution studies were conducted in pH 6.8 phosphate buffer using USP apparatus XXIV. Result and Discussion: Results showed uniform tablet mass and favorable powder mixture flowability, ensuring ODT physical properties. Tablets exhibited excellent mechanical resistance with consistent hardness and low friability loss. All formulations demonstrated high and uniform drug content. Different superdisintegrants influenced wetting, disintegration, and dissolution times. Crospovidone exhibited the fastest wetting time but longer disintegration times, attributed to increased tablet hardness. Dissolution studies revealed that crospovidone-containing ODTs had faster drug release compared to croscarmellose sodium and sodium starch glycolate, aligning with literature findings. The study emphasized the importance of considering both wetting and disintegration times for a comprehensive evaluation of ODT performance. Croscarmellose sodium and sodium starch glycolate hindered drug release, forming gel-like masses impeding dissolution, while crospovidone enhanced drug release in formulated ODTs. In conclusion, the study provides valuable insights for pharmaceutical development and patient-centric drug delivery solutions, showcasing the influence of superdisintegrants on ODT performance and emphasizing the importance of considering various parameters for comprehensive evaluation.

Rifaximin, a broad-spectrum antibiotic, boasts a unique chemical composition and pharmacokinetic profile, rendering it highly effective in treating irritable bowel syndrome (IBS). Its minimal systemic absorption confines its impact to the gastrointestinal (GI) tract, where it yields significant therapeutic benefits. This review examines rifaximin's physico-chemical attributes and its role in managing IBS symptoms. Its molecular structure facilitates intestinal lumen retention postoral administration, minimizing systemic exposure and adverse effects. This targeted action is crucial in addressing the gut microbiota's role in IBS pathophysiology. By modifying microbial populations and their metabolite production, rifaximin mitigates symptoms like bloating, irregular bowel habits, and abdominal pain associated with IBS. It achieves this by reducing pathogenic bacteria and altering bacterial metabolism, enhancing mucosal and immune function. Clinical trials affirm rifaximin's superiority over placebo and conventional therapies in alleviating overall IBS symptoms and addressing small intestine bacterial overgrowth (SIBO). Despite its promising efficacy and sustained symptom relief, further research is essential to optimize long-term effectiveness and dosing regimens. Rifaximin stands as a vital treatment option for IBS due to its distinctive properties and clinical utility; yet, ongoing investigation is imperative for maximizing its therapeutic benefits.

Quality by design (QbD) provides a new approach to pharmaceutical quality. This chapter provides extensive information on pharmaceutical QbD and how it can be used to ensure the quality of pharmaceuticals. In addition, the components of quality with design and the advantages, opportunities, and steps provided by quality with design are summarized. Pharmaceutical development aims to create a high-quality product and manufacturing method that consistently delivers the expected performance of the product. Quality cannot be tested into items, but it should be designed into them. It contains the quality goal product profile, critical quality attributes, and significant QbD features. It also compares product quality based on end-of-life testing to product quality based on QbD. The ICH Guidelines serve as the foundation for QbD. It is based on the ICH Guidelines Q8 and Q9 for pharmaceutical development, as well as Q10 for pharmaceutical quality systems. One of the most fundamental steps of QbD, design of experiment (DoE) analysis is used to significantly reduce the number of experiments required to build a model design space. The right tools for design space development are determined from many aspects, including the complexity of the system under study and scientific data. Therefore in this chapter, the basic steps, principles, and types of experimental design are discussed in detail. As a result, this chapter has the feature that can be useful for any researcher who wants to know about QbD, which enables effective, efficient, and economical production in the field of pharmaceutical production.

Colon-targeted drug delivery systems have garnered significant interest as potential solutions for delivering various medications susceptible to acidic and catalytic degradation in the gastrointestinal (GI) tract or as a means of treating colonic diseases naturally with fewer overall side effects. The increasing demand for patient-friendly drug administration underscores the importance of colonic drug delivery, particularly through noninvasive methods like nanoparticulate drug delivery technologies. Such systems offer improved patient compliance, cost reduction, and therapeutic advantages. This study places particular emphasis on formulations and discusses recent advancements in various methods for designing colon-targeted drug delivery systems and their medicinal applications.

Pharmaceutical excipients are indispensable components of drug formulations, playing critical roles in enhancing stability, improving bioavailability, and ensuring patient compliance. In pediatric and geriatric populations, the selection of these excipients becomes even more crucial due to their unique physiological and pharmacokinetic profiles, as well as age-specific formulation requirements. This review examines the functions, safety considerations, and potential adverse effects of excipients in these vulnerable groups. It addresses the challenges of drug formulation for neonates, infants, and elderly patients, including immature enzyme systems, polypharmacy, and swallowing difficulties. The impact of excipient-excipient and excipient-active pharmaceutical ingredient (API) interactions on drug stability, efficacy, and safety is also highlighted. For instance, the effects of polyethylene glycol (PEG) in patients with impaired renal function and destabilizing interactions between surfactants and protein-based APIs are analyzed. Additionally, current guidelines and safety requirements from regulatory bodies such as the FDA, EMA, and ICH are reviewed. This paper emphasizes the importance of carefully selecting excipients that balance functionality and safety to ensure therapeutic efficacy while minimizing risks for pediatric and geriatric patients. Future directions in excipient development and formulation strategies are also discussed to improve treatment outcomes for these populations.

This study aimed to assess and compare diverse formulations of ivermectin-loaded liposomes, employing lipid film hydration and ethanol injection methods. Three lipids (DOPC, SPC, and DSPC) were used in predetermined molar ratios. A total of 18 formulations were created, and a factorial design determined the optimal formulation based on particle size, polydispersity index (PDI), zeta potential, and encapsulation efficiency. The average mean particle size, PDI and zeta potential of the selected formulations (F1, F2, F7, F9, and F11) was, respectively, 196.40 ± 44.60 nm, 0.39 ± 0.09, and -40.24 ± 9.17. The encapsulation efficiency exceeded 80%, with a mean loading capacity of 4.00 ± 1.70%. In vitro studies included transmission electron microscopy, Fourier transform infrared spectroscopy, drug release, and antiviral activity assessments against SARS-CoV-2. The liposomal formulations demonstrated superior antiviral activity compared to free ivermectin, as indicated by lower IC50 values. The results of this study emphasize the effectiveness of ivermectin-loaded liposomes in inhibiting viral activity, highlighting their potential as promising candidates for antiviral therapy. The findings suggest that the strategic use of liposomes as drug carriers can significantly modulate and improve the antiviral properties of ivermectin, offering a novel approach to harnessing its full therapeutic potential. Collectively, these results provide a robust foundation for further exploration of ivermectin as a viral protection tool and optimization of its delivery mechanisms.