18 research outputs found
Lipid nanoparticles: Different preparation techniques, characterization, hurdles, and strategies for the production of solid lipid nanoparticles and nanostructured lipid carriers for oral drug delivery
No full textTHE AI REVOLUTION IN PHARMACEUTICALS: INNOVATIONS, CHALLENGES, AND FUTURE PROSPECTS – AN OVERVIEW
No full textArtificial intelligence (AI) is transforming pharmaceutical research and development (R and D), and making measurable improvements in efficiency, precision, and cost-effectiveness in drug research and development. AI-enabled platforms have cut the drug discovery pipeline timelines in comparison to the traditional 4-6 y down to 46 d, along with speeding up compound screening by 1-2 y and reduced clinical trial duration by up to 59% and increased the accuracy of patient selection 80-90%. In formulation optimization artificial neural networks, neuro--fuzzy systems, and hybrid model-based AI models have been able to predict dissolution profile and critical quality attributes with accuracy rates of over 90%, with 30-50% lower experimental workload. In this review, the cross-domain evidence on the use of AI in the continuum of target identification to regulatory integration is thoroughly synthesized and critical evaluations on existing limitations which include data bias, interpretability discrepancy and regulatory ambiguity discussed. It proposes a systematized framework of integration, which places the emphasis on creating high impact pilot projects, in-the-wild testing and further monitoring or observing of models according to the instructions of FDA, EMA and EU AI Act. Synthesizing measures of quantitative values along with practical measures, the present work offers a blueprint of unambiguously converting the ideological potential of AI into implementable, regulator-compatible utilities in pharmaceutical science
Dissolving Microneedles in Therapeutics: A Smart Approach to Minimally Invasive Drug Delivery
No full text Current developments in the field of transdermal drug delivery have placed the dissolving microneedles (DMNs) technology on the path to changing the landscape of taking medicine as an aspect of painless, self-administered, physio-minimally invasive, and contrasted to normal subcutaneous or intramuscular injections. In this review, the DMN systems evolution is followed, and the formation of these systems as drug carriers to multifunctional platforms that can be used in various types of diseases has been outlined. The importance of fabricating DMNs through techniques (micromolding, droplet-born air blowing, and drawing lithography) is discussed in detail considering attaining structural integrity and fast dissolution. The incorporation of biocompatible materials as polymers, e.g., hyaluronic acid, polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA), carboxymethyl cellulose (CMC), and chitosan (CS), is considered in terms of maximizing the mechanical strength aspects, rate of dissolution. Skin penetration efficiency, bioavailability of the drug, and stability in the physiological environment are covered by performance testing. Although DMNs hold great potential for clinical benefits such as increased patient compliance and decreased risk of infection, there are still concerns about large-scale production and formulation standardization and regulatory acceptance. These are the obstacles that have to be considered in the process of successful translation of DMNs into routine work.
KEYWORDS
Dissolving microneedle, transdermal drug delivery, biodegradable polymers, Minimally invasive systems, controlled drug release
Formulation and Evaluation of a Biocompatible Natural Sunscreen Cream Containing Compritol 888 ATO and Essential Oils
No full text Background: Natural sunscreens are increasingly preferred due to their biocompatibility, antioxidant activity, and safety for sensitive skin. Plant-based oils and mineral ultraviolet filters offer multifunctional benefits and broad-spectrum protection, aligning with current demands for eco-friendly skincare.
Objective: To formulate and evaluate a stable, natural sunscreen cream using Compritol 888 ATO, carrot seed oil, rosemary essential oil, and zinc oxide for enhanced photoprotection and skin compatibility. Methods: Three formulations (F1, F2, F3) were prepared with varying concentrations of natural actives. Evaluation included pH, spread ability, viscosity, stability, irritancy, and washability. In-vitro sun protection factor values were determined using Mansur’s method, measuring ultraviolet absorbance from 290 to 320nm.
Results: All formulations had skin-compatible pH (6.2-6.6), smooth texture, and good spread ability (up to 14.9 g.cm/sec). No irritation or rancidity was observed. F3, the optimized formulation, showed the highest viscosity (16,950 cP), best stability, and an SPF of 13.82. The synergistic effects of carrot seed and rosemary essential oils, rich in natural antioxidants, along with zinc oxide’s broad-spectrum blocking ability, contributes to improved ultraviolet protection. Compritol 888 ATO played a critical role in emulsion stability and enhanced application. Conclusions: The developed natural sunscreen cream demonstrated excellent photoprotective efficacy, physicochemical stability, and biocompatibility. These findings support the use of natural oils and mineral filters in effective, skin-safe, and sustainable sun care products.
KEYWORDS
Natural sunscreen, sun protection factor, carrot seed oil, rosemary essential oil, Compritol 880 ATO, zinc oxide, photoprotection
A Systematic Study on Long-acting Nanobubbles: Current Advancement and Prospects on Theranostic Properties
No full textDelivery of diagnostic drugs via nanobubbles (NBs) has shown to be an emerging field of study. Due to their small size, NBs may more easily travel through constricted blood vessels and precisely target certain bodily parts. NB is considered the major treatment for cancer treatment and other diseases which are difficult to diagnose. The field of NBs is dynamic and continues to grow as researchers discover new properties and seek practical applications in various fields. The predominant usage of NBs in novel drug delivery is to enhance the bioavailability, and controlled drug release along with imaging properties NBs are important because they may change interfacial characteristics including surface force, lubrication, and absorption. The quick diffusion of gas into the water was caused by a hypothetical film that was stimulated and punctured by a strong acting force at the gas/water contact of the bubble. In this article, various prominent aspects of NBs have been discussed, along with the long-acting nature, and the theranostical aspect which elucidates the potential marketed drugs along with clinical trial products. The article also covers quality by design aspects, different production techniques that enable method-specific therapeutic applications, increasing the floating time of the bubble, and refining its properties to enhance the prepared NB’s quality. NB containing both analysis and curing properties makes it special from other nano-carriers. This work includes all the possible methods of preparing NB, its application, all marketed drugs, and products in clinical trials
NASAL IN-SITU GEL DRUG DELIVERY SYSTEMS FOR OSTEOPOROSIS: ADVANCES IN THERMORESPONSIVE AND MUCOADHESIVE FORMULATIONS
No full textOsteoporosis is a chronic metabolic bone disorder requiring sustained pharmacotherapy. Conventional oral drugs such as raloxifene and bisphosphonates are limited by poor bioavailability, gastrointestinal intolerance, and poor patient compliance. Nasal in-situ gel drug delivery systems represent a thrilling alternative by combining the advantages of the nasal route with the application of temperature-sensitive and mucoadhesive polymers to enhance drug absorption and residence time. This review emphasizes recent progress in nasal in-situ gel formulation for osteoporosis treatment, with attention to formulation approaches, pharmacokinetics, efficacy, safety, and regulatory aspects. The studies have shown increased systemic bioavailability (up to 13.4-fold for raloxifene), increased bone mineral density, and non-irritating, stable formulations appropriate for long-term administration. Further, employing FDA-approved drugs and GRAS-listed excipients allows development through the 505(b)(2) regulatory route. Although formulation achievement is met, limitations of nasal volume, mucosal tolerability, and clinical translatability still exist. Nasal in-situ gels are well-positioned to be non-invasive, scalable candidates for efficacious osteoporosis treatment.
KEYWORDS
Nasal In-situ gel, Osteoporosis, Raloxifene, Bisphosphonates, Mucoadhesive polymers, Thermoresponsive delivery, Bioavailability enhancement, Drug delivery system, GRAS excipients, 505(b)(2) pathway
STANDARDIZATION OF AN AYURVEDIC POLYHERBAL LIQUID FORMULATION WITH IMPROVED PALATABILITY FOR THE MANAGEMENT OF ANEMIA
No full textObjective: This study aimed to develop and standardize a palatable Ayurvedic polyherbal oral liquid formulation for anaemia treatment. By integrating taste-masking techniques, the aim is to enhance iron absorption, reduce side effects, and improve patient adherence.
Methods: Four iron-rich Ayurvedic herbs, namely Punica granatum, Vitis vinifera, Boerhaavia diffusa, and Terminalia bellirica, were extracted and formulated with taste-masking excipients. The syrup formulation involved hydroalcoholic extraction, freeze-drying, and stability testing under accelerated and long-term conditions. Standardization parameters included organoleptic evaluation, physicochemical assessment, microbiological testing, and heavy metal residue analysis.
Results: The hydroalcoholic extraction of Terminalia bellirica fruit yielded 17.3%, while Boerhavia diffusa root extract yielded 9.3%. Freeze-dried fruit juices of Vitis vinifera and Punica granatum yielded 8.6% and 7.3%, respectively. A polyherbal syrup was formulated and optimized through six trials, balancing taste, viscosity (120–146 cP), and stability. The final formulation contained 12.5 mg iron per 5 ml, with synergistic herbal components enhancing bioavailability. Sensory evaluations confirmed improved palatability and stability studies demonstrated a prolonged shelf life. Heavy metal analysis confirmed compliance with safety standards, ensuring the formulation\u27s suitability for anaemia management.
Conclusion: This Ayurvedic polyherbal liquid formulation, with its enhanced taste profile and iron-rich content, offers a novel and patient-friendly approach to anaemia management. Its improved palatability may enhance patient compliance, particularly in populations struggling with conventional iron supplements. Moreover, its formulation aligns with the growing demand for natural, well-tolerated therapeutic alternatives, underscoring its potential for commercialization. Further clinical studies are recommended to validate its efficacy, long-term safety, and market viability for broader therapeutic application
NANOPARTICLE-EMBEDDED MICRONEEDLES FOR ENHANCED TRANSDERMAL DELIVERY: ADVANCES AND APPLICATIONS
No full textTransdermal drug delivery (TDD) provides a non-invasive alternative to oral and injectable administration, avoiding gastrointestinal degradation and first-pass metabolism. Traditional TDD systems are limited to small, lipophilic drugs and are prone to skin irritation and low bioavailability. Although microneedles (MNs) have several advantages, they also suffer from limited drug-loading capacity, fast drug diffusion, and mechanical fragility. Recent developments combine nanoparticles with microneedles (NEMNs), improving drug stability, bioavailability, and controlled release. The types of MNs (solid, coated, hollow, dissolving, and hydrogel) and considerations regarding materials (silicon, metals, polymers) are presented alongside nanoparticles to enhance therapeutic outcomes. Advancements in manufacturing methods, such as 3D printing and micro molding, have facilitated the controlled deposition of nanoparticles and enabled scalable fabrication. Stimuli-induced NEMNs triggered by pH, glucose, light, and magnetic fields have applications in site-specific drug release for diabetes management, cancer treatment, wound healing, and the treatment of inflammatory ailments. Combining nanomaterials with biodegradable polymers enhances their strength and compatibility with living organisms. Although improvements have been made, nanoparticle stability, scalability, regulatory compliance, and long-term safety remain significant concerns. To encourage clinical translation, future directions will focus on AI-based closed-loop systems, biomaterials that can perform multiple functions, and eco-friendly manufacturing processes. Overcoming these barriers, NEMNs have the potential to serve as patient-centric treatments for both chronic and acute conditions, thereby closing the gap between nanotechnology and minimally invasive therapeutics
DEVELOPMENT OF GUGGULSTERONE-LOADED PHYTOSOMES: A QUALITY BY DESIGN-BASED CHARACTERIZATION AND OPTIMIZATION STUDIES
No full textObjective: The primary objective of this study was to enhance drug delivery efficiency through the design and optimization of guggulsterone-pyrosomes, employing a 3-factor, 3-level box-behnken design.
Methods: The methodology involved a solvent evaporation technique utilizing guggulsterone and soy lecithin, with a systematic variation and optimization of critical factors such as soy lecithin and guggulsterone concentration, alongside temperature adjustments to refine the phytosome formulations. The characterizations of these formulations were extensive, with a particular emphasis on key quality attributes, notably percentage entrapment efficacy and drug release.
Results: The optimized guggulsterone-pyrosomes demonstrated impressive outcomes, showcasing a remarkable entrapment efficiency of 92.64% and a noteworthy drug release rate of 91.69% at 24 h. These formulations displayed heightened viability in selected cell lines, exhibiting cellular toxic c concentrations ranging from 253.39 to 330.44 µg/ml. Moreover, they exhibited stability under stressed conditions from a physicochemical perspective. The particle size was measured at 137.8 nm, with a zeta potential of-25.3 mV.
Conclusion: Significantly, the extended drug release from guggulsterone-pyrosomes adhered to first-order kinetics with Fickian diffusion. In summary, this study underscores the efficacy of the box-behnken design in crafting optimized guggulsterone-pyrosomes, showcasing their potential as promising drug delivery carriers. The enhanced drug delivery platform exhibits significant promise in amplifying antihyperlipidemic effects, attributed to the improved performance and stability of these innovative phytosome
DEVELOPMENT AND CHARACTERIZATION OF TACROLIMUS TABLET FORMULATIONS FOR SUBLINGUAL ADMINISTRATION
No full textObjective: The study aimed to prepare and characterize inclusion complexes of tacrolimus with β-cyclodextrin to improve its solubility and to formulate them into sublingual fast disintegrating tablets with a view to bypass the first-pass metabolism.
Methods: Tacrolimus: β-cyclodextrin inclusion complexes (1:1 and 1:2 molar proportions) were prepared using the kneading method. Their characterization was accomplished by determining the drug content, solubility, Attenuated Total Reflection-Infrared Spectroscopy (ATR-IR), Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), and powder X-Ray Diffraction analysis (pXRD). These were then formulated to fast disintegrating tablets and evaluated for precompression as well as post compressional characteristics.
Results: SEM analysis showed the inclusion complexes as rough, non-porous, irregular surfaced aggregate particles. DSC and pXRD analyses confirm the crystallinity change and partial conversion to the amorphous form of the drug in the inclusion complexes. From the solubility studies, it was observed that both the inclusion complexes of 1:2 molar ratio (14.82±0.889 µg/ml) and 1:1 molar ratio (12.72±0.1004 µg/ml) improved the aqueous solubility to greater extents in comparison to that of the pure drug (3.05±0.121 µg/ml). All the tablet formulations showed good precompression and mechanical properties. The inclusion complex loaded tablets exhibited a superior drug release pattern when compared to tablets prepared with tacrolimus alone. The optimized formulation (TT3) showed an in vitro disintegration time of 34.33 s and a percent drug release of 97.87.
Conclusion: The inclusion complex formulation combined with the sublingual route of administration can be expected to result in an improved bioavailability of tacrolimus by increasing its solubility and bypassing first-pass metabolism
