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We undertook this study to determine the safe limits of capsulorhexis during nucleus expression in 40 eyes of patients undergoing extracapsular cataract extraction (ECCE) with a posterior chamber intraocular lens (PC IOL) implantation and in 30 cadaver eyes. In group I (patient eyes), capsulorhexis of 4.5 to 7.5 mm was performed and the nucleus was expressed by hydrodissection. The nuclei measured 4.5 to 9.0 mm. One relaxing incision at 12 o′clock position had to be placed in 9 patients. In group II (cadaver eyes), continuous curvilinear capsulotomies of 4.0, 4.5, 5.0, 5.5, 6.0 and 6.5 mm were made in 5 eyes each. No relaxing incisions were placed. In both the groups, nuclei of all sizes could be safely delivered through intact capsulotomies measuring 5.5 mm or more. In two patient eyes, posterior capsule rupture occurred with rhexis measuring 4.5 and 5.0 mm, respectively. In the cadaver eyes, intracapsular extraction occurred in 4 eyes with rhexis measuring 5.0 mm or less. We conclude that a rhexis less than 5.5 mm is not safe for nucleus delivery during ECCE.

Objective: The objective of this study is to create predictive models utilizing machine learning algorithms, including Artificial Neural Networks (ANN), k-nearest neighbor (kNN), support vector machines (SVM), and linear regression, to predict critical quality attributes (CQAs) such as hardness, friability, and disintegration time of fast disintegrating tablets (FDTs). Methods: A dataset of 864 batches of FDTs was generated by varying binder types and amounts, disintegrants, diluents, punch sizes, and compression forces. Preprocessing steps included normalizing numerical features based on industry standards, one-hot encoding for categorical variables, and addressing outliers to ensure data consistency. Four machine learning models were trained and evaluated on R2 values and mean squared error (MSE). Feature importance was analyzed using permutation importance, and statistical validation (p < 0.05) and confidence intervals were computed for model performance. The 'differential_evolution' function was used to optimize the formulation. Results: Among the models, ANN demonstrated the highest predictive accuracy, achieving R2 values up to 0.9550 with the lowest MSE across training and test datasets, outperforming kNN, SVM, and linear regression. The ANN's ability to model complex, non-linear interactions between formulation variables was statistically significant, as validated through six checkpoint batches of acetylsalicylic acid FDTs. The feature importance analysis revealed compression force, binder type, and punch size as the most influential factors affecting hardness, while disintegrant type influenced friability. The 'differential_evolution' function effectively optimized the CQAs, resulting in FDTs with ideal characteristics. Conclusion: The ANN model, integrated with differential evolution, provided a robust tool for optimizing FDT formulations by accurately predicting CQAs and reducing the need for extensive experimental trials. Compared to traditional optimization methods, ANN excels in capturing intricate multi-variable relationships, making it a valuable approach for scaling beyond acetylsalicylic acid to other formulations. This method enhances the consistency and efficiency of tablet formulation, supporting broader pharmaceutical applications [ABSTRACT FROM AUTHOR]

Darunavir has a low oral bioavailability (37%) due to its lipophilic nature, metabolism by cytochrome P450 enzymes and P-gp efflux. Lipid nanoparticles were prepared in order to overcome its low bioavailability and to increase the binding efficacy of delivery system to the lymphoid system. Darunavir-loaded lipid nanoparticles were prepared using high-pressure homogenization technique. Hydrogenated castor oil was used as lipid. Peptide, having affinity for CD4 receptors, was grafted onto the surface of nanoparticles. The nanoparticles were evaluated for various parameters. The nanoparticles showed size of less than 200 nm, zeta potential of − 35.45 mV, and a high drug entrapment efficiency (90%). 73.12% peptide was found conjugated to nanoparticles as studied using standard BSA calibration plot. Permeability of nanoparticles in Caco-2 cells was increased by 4-fold in comparison to plain drug suspension. Confocal microscopic study revealed that the nanoparticles showed higher uptake in HIV host cells (Molt-4 cells were taken as model containing CD4 receptors) as compared to non-CD4 receptor bearing Caco-2 cells. In vivo pharmacokinetic in rats showed 569% relative increase in bioavailability of darunavir as compared to plain drug suspension. The biodistribution study revealed that peptide-grafted nanoparticles showed higher uptake in various organs (also in HIV reservoir organs namely the spleen and brain) except the liver compared to non-peptide-grafted nanoparticles. The prepared nanoparticles resulted in increased binding with the HIV host cells and thus could be promising carrier in active targeting of the drugs to the HIV reservoir. [ABSTRACT FROM AUTHOR]

Colon-targeted capecitabine beads were formulated by an ionotropic gelation method. The sodium alginate to pectin ratio and chitosan concentration were optimized using a 32full factorial design. Analysis of response surface plots allowed the identification of an optimized formulation with high drug entrapment and controlled release. Insignificant differences in observed and predicted values for responses validated the optimization method. Optimized beads possessed an average diameter of 1395 µm and good flow properties. Their production as spherical beads having a smooth surface was confirmed by scanning electron microscopy. Fourier transform infrared spectroscopy revealed the compatibility of drug with added excipients, while differential scanning calorimetry study confirmed complete drug entrapment in polymer matrix. Higher swelling of beads in phosphate buffer pH 7.4 was obtained in comparison to pH 6.8. An in vitro wash off test indicated 70% mucoadhesion by the beads. In vitro dissolution studies of beads loaded into enteric-coated capsules revealed negligible release in simulated gastric and intestinal fluid, followed by 49.23% release in simulated colonic fluid, in 4 h. The optimized beads were found to be stable for three months at 25 ± 2°C/60 ± 5% RH. In conclusion, the formulated beads showed colon-specific controlled release properties, and thus could prove to be effective for colon cancer treatment. [ABSTRACT FROM AUTHOR]

Since ancient times, mouth fresheners in many different forms have been used throughout the world. Traditional knowledge describes the health benefits of mouth fresheners, and contemporary science is now investigating their benefits. Claims have been made that mouth fresheners not only improve digestion but also promote oral health. Similar, but in a more profound sense, probiotics offer astounding advantages in treating many disorders. In certain cases, probiotics also offer prophylactic effects. Numerous benefits for dental health are being studied for B. coagulans (MB-BCM9) and B. subtilis (MB-BSM12). In this current study, a probiotic and a mouth freshener were combined to ameliorate the impacts of both. The oral residence of probiotics was enhanced by employing mucoadhesive polymers. Numerous compositions were developed and evaluated for the unaltered growth of probiotics, along with other evaluations like microscopy, in vitro mucoadhesive strength, and stability studies. Xanthan gum and hydroxypropyl methylcellulose were used in the development of mucoadhesive probiotic powder by employing the lyophilization technique. More than five hours of residence time were observed in the in vitro study with goat oral mucosa. The enumeration study validated the label claims of MB-BCM9 and MB-BSM12. It also concluded that none of the components of the formulation had a detrimental effect on probiotics. In essence, the present work discloses the novel and stable formulation of a probiotic-based mouth freshener., (Copyright© by International Journal of Pharmaceutical Compounding, Inc.)

In present investigation, novel physiologically activated phase transition systems for Ketorolac Tromethamine was developed. In-situ gelling systems: pH sensitive gel using carbopol 980 and HPMC K100LV, ion sensitive gel using gallan gum and temperature sensitive gel using Poloxamer 407 and Poloxamer 188 were developed. The drug content, content uniformity, pH, optical transmittance, rheological property, bioadhesive strength, in-vitro drug release, ocular irritation and stability study were evaluated. Characterization revealed that gels were conforming to all criteria required for ocular delivery in terms of stability on sterilization, long residence time, non-irritability and sustained drug release without affecting vision. Thus, In-situ gels can be a promising alternative to the prevalent market formulations.

The aim of the present work was to formulate a self-microemulsifying drug delivery system (SMEDDS) containing orlistat. The oil, surfactant and co-surfactant were decided based on the solubility studies. Pseudoternary phase diagrams were plotted, microemulsification area was determined and different formulations were prepared. Particle size, zeta potential, dispersibility test and thermodynamic stability studies were measured. In-vitro dissolution test of thermodynamically stable formulations OS-B and OS-C were carried and results were compared with those of plain drug and suspension formulation. Stability studies performed indicated that formulation OS-C remained stable over 12 months period. Thus this investigation concluded that hydrophobic drugs like orlistat can be delivered effectively through the formulation of SMEDDS.