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Abstract Dorzolamide hydrochloride (DRZ) is a carbonic anhydrase inhibitor utilized in managing elevated intraocular pressure (IOP) associated with glaucoma. However, its clinical effectiveness is hindered by a short half-life, low residence time, and the need for frequent dosing, highlighting the necessity for innovative delivery systems. This work reviews recent advancements in DRZ delivery, particularly focusing on cyclodextrin complexation and nanotechnology applications. It explores the potential of cyclodextrin derivatives to enhance DRZ’s bioavailability. DRZ cyclodextrin complexes or nanoparticulate systems maintain high drug concentrations in the eye while minimizing irritation and viscosity-related issues. Nanotechnology introduces nanoparticle-based carriers such as polymeric nanoparticles, solid lipid nanoparticles, liposomes, niosomes, and nanoemulsions. These formulations enable sustained drug release, improved corneal permeation, and enhanced patient compliance. Clinical trials have shown that DRZ nanoparticle eye drops and nanoliposome formulations offer efficacy comparable to conventional therapies, with the potential for better tolerability. Overall, this review highlights significant progress in DRZ delivery systems, suggesting their potential to transform glaucoma treatment by addressing current limitations and improving therapeutic outcomes.

Introduction: Olanzapine (OLZ) is a psychotropic class drug commonly used to treat schizophrenia, bipolar disorder, and acute manic episodes. It has less water solubility, resulting in a slow dissolution rate and oral bioavailability. Therefore, the development in oral dosage forms is required to enhance the drug solubility. Method: The solid dispersion of olanzapine is prepared by spray drying technique. The solution of polyvinylpyrrolidone K-30 (PVP K-30), mono amino glycyrrhizinate pentahydrate (GLY), OLZ and silicon dioxide were dissolved in distilled water and ethanol and spray dried to get the solid dispersion. Solid dispersion was characterized for surface morphology, solubility, encapsulation efficiency (EE), X-ray diffraction (X-RD), Differential Scanning Calorimeter (DSC) and drug-polymer interaction by Fourier transforms infrared spectroscopy. Results: The amorphous nature of the drug's incorporation in solid dispersion was confirmed by X-RD analysis. Prepared solid dispersion showed higher solubility, 11.51 mg, than pure OLZ (0.983 mg ml-1), while the range of EE was found to be between 64 to 90 %. Conclusions: The solubility and dissolution rate of the OLZ can effectively increase by spray-dried solid dispersion. Plackett–Burman screening design plays a vital role in understanding the effect of independent variables on EE and solubility.

Abstract Background The development of chromatographic method and the validation of a sensitive, simple, efficient, and reversed-phase high-performance liquid chromatography (RP-HPLC) approach were adopted for the drug flurbiprofen (FBP) in nanoparticles formulation by using a design of experiment (DoE). The critical method variables (CMVs) were screened using a statistical two-level fractional factorial design (FFD) followed by optimization of the selected CMVs that influence the analytical responses (ARs) of the RP-HPLC process by using two-level full factorial design. Results Statistical models are used to investigate the effects of system factors including column temperature, flow rate, and methanol in orthophosphoric acid (OPA) on the dependent responses, retention time, peak area, tailing factor, and theoretical plates in HPLC. The ideal column temperature (25 °C), flow rate (1 ml/min), and mobile phase (methanol 85 percent v/v in 0.05 percent OPA in water) were selected independently from the response surface at three levels (1, + 1, and 0) for further validation at constant solvent pH 2.75. Optimized method in the RP-HPLC resulted a retention time of 4.75 min, a peak area of 3975.12, a tailing factor of 0.73, and a total of 9697.7 theoretical plates followed by validation in accordance with the current ICH recommendations Q2 (R1). Linearity, precision, accuracy, assay, limit of detection (LOD), limit of quantification (LOQ), and robustness were all included in validation. The calibration curve was linear (r 2 = 0.9997, slope = 70.72) for the concentration of 10 to 50 µg/ml, with a limit of detection of 0.14 µg/ml. Furthermore, stability-indicating methods demonstrate that drug degradation is highest in the presence of basic circumstances (about 96.49%), followed by oxidation (about 76.41%), and acidic conditions (about 48.12%), whereas drug is stable in some extent under neutral, photo (sunlight), and dry heat conditions. Conclusions Effect of independent variables on dependent responses was screened and optimized by using statistical software design. A method for drug development could be successfully implemented for the estimation of drug in nanoparticles formulation as well as for the routine analysis in bulk and pharmaceutical formulations. The high recovery and low relative standard deviation support the suitability of proposed method that could be employed. Graphical Abstract

The graph of drug resistance in cancer is reportedly increasing in terms of therapeutic efficiency. As per the WHO reports, around 70% of death reported in low- and middle-income countries. The increase in death toll was imparted from improper diagnosis and inadequate therapy. The 25% increase in disease burden may be laden due to resistance mutations in cancer during treatment. Exposure of high concentrations of chemotherapeutic agents leads to toxicity in the normal cells. Long-term conventional chemotherapy develops acquired resistance. The conventional therapeutics was not able to target the cancer cell specifically and need to promulgate the use of nanocarrier or bioengineering for the polychemotherapy. Phytochemicals are natural constituents providing alternative therapeutic approach to minimize the resistance. The present review highlights the nano-therapeutic approaches pondering over the conventional chemotherapy. The phytochemicals are extracted, isolated, and purified from daily dietary fibers or natural plants. Natural extractives act via multiple pathways and provide optimum effectiveness against resistance cancer. The poor solubility and bioavailability are major constraints in combination therapy. The nanotechnological approach improves the functional properties transportation across cell barriers, and improves bioavailability. The present review highlights the phytochemical based nanoformulations in improving the therapeutic response and several alternative ways to target resistance cancer. The major implications of phytochemical and chemotherapeutic combination therapy could lead in the future.

Abstract This work mainly focuses on the graphene oxide (GO)‐assisted sustainable drug delivery of famotidine (FMT) drug. Famotidine is loaded onto GO and encapsulated by chitosan (CH). UV‐visible spectroscopy, field emission scan electron microscopy, and atomic force microscopy confirm the loading of FMT on GO. An interaction of FMT with GO and CH through amine functionalities is confirmed by Fourier‐transform infrared spectroscopy. Differential scanning calorimetric and cyclic voltammetric investigations confirm the compatibility of FMT and its retaining activity within chitosan‐functionalized graphene oxide (CHGO) composite. Encapsulation efficiency of FMT is determined for various CHGO‐FMT combinations and found to be higher at 1:9 ratio. The in vitro drug release profile is studied using a dissolution test apparatus in 0.1 m phosphate buffer medium (pH = 4.5), which shows sustainable drug release up to 12 h, which is greater than the market product (Complete release within 2 h). Comparative study of drug encapsulated with CH and without GO elucidates that GO is responsible for the sustainable release. The “n” value obtained from slope using Korsmeyer–Peppas model suggests the super case‐II transport mechanism.

The objective of this study was to prepare diclofenac sodium loaded microparticles by single emulsion [oil-in-water (o/w)] solvent evaporation method. The 22 experimental design methodology was used to evaluate the effect of two formulation variables on microspheres properties using the Design-Expert® software and evaluated for their particle size, morphology, and encapsulation efficiency and in vitro drug release. The graphical and mathematical analysis of the design showed that the independent variables were a significant effect on the encapsulation efficiency and drug release of microparticles. The low magnitudes of error and significant values of R2 prove the high prognostic ability of the design. The microspheres showed high encapsulation efficiency with an increase in the amount of polymer and decrease in the amount of PVA in the formulation. The particles were found to be spherical with smooth surface. Prolonged drug release and enhancement of encapsulation efficiency of polymeric microparticles can be successfully obtained with an application of experimental design technique.

Nanogels are submicron-size aqueous dispersions of water-swollen particles, composed of nano-sized three-dimensional highly cross-linked networks of hydrophilic polymers. An active pharmaceutical agent or therapeutic agent with high or low molecular weight can be easily encapsulated into nanogels that can be delivered to the site of action via various routes, including oral, pulmonary, nasal, parenteral and intraocular routes, among others. Therapeutic agents encapsulated into nanogels improve the therapeutic activity in the biological environment. The application of different nanogels in drug delivery and recent clinical trial studies has been described concisely in this review.

The purpose of this study was to prepare polymeric microspheres containing Ketoprofen (KFN) by single emulsion [oil-in-water (o/w)] solvent evaporation method. Polycaprolactone (PCL), biocompatible polymer, was used for the preparation of sustained released microspheres of KFN. A Plackett–Burman design was employed by using the Design-Expert® software (Version- 9.0.3.1, Stat-Ease Inc., Minneapolis, MN). Eleven factors out of six processing factors were investigated in order to enhance the encapsulation efficiency (EE) of the microspheres. The resultant microspheres were characterized for their size, morphology, EE, and drug release. Imaging of particles was performed by field emission scanning electron microscopy. Interaction between the drug and polymers were investigated by Fourier transform infrared (FTIR) spectroscopy, X-ray powder diffractometry (XRPD) and Differential Scanning Calorimetry (DSC). Graphical and mathematical analyses of the design showed that concentration of factor PCL (B) and varying speed (F, revolution per minute, rpm) were significant negative effect on the EE and identified as the significant factor determining the EE of the microspheres. The microspheres showed high % EE (31.18 % to 96.81 %). The microspheres were found to be discrete, oval with porous surface. The FTIR analysis confirmed no interaction of KFN with the polymer. The XRPD revealed the dispersion of drug within microspheres formulation. Sustained drug release profile over 12 h was achieved by PCL polymer. In conclusion, polymeric microspheres containing KFN can be successfully prepared using the technique of experimental design, and these results helped in finding the optimum formulation variables for EE of microspheres.