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BACKGROUND: Estimation of the drug and development of the method is a critical aspect of formulation development and a critical factor for analytical scientists. Gefitinib is a poorly soluble anticancer drug. OBJECTIVE: The present research focuses on the topic of the development of innovative quality by design methods for the estimation of gefitinib (GF) from bulk, pharmaceutical tablet formulation, and complex nanoformulations. METHODS: To simplify the estimation of poorly soluble drugs such as GF, response surface methodology (RSM) was adopted with effective leverages to obtain precise computation design space using the Box-Behnken design (BBD) model. The major three mixed-effect independent factors (percentage of buffer, pH of buffer, and flow rate) were screened with three prominent dependent responses (viz., theoretical plate, retention time, and tailing factor) selected for optimal analysis. Furthermore, co-processed steps were employed for the estimation of the analyte from the complex formulation. RESULTS: The RP-HPLC method uses the quality by design (QbD) approach can effectively estimate the analyte concentration of less than 4.5 min. The developed method was economically robust and sensitive and shows a relative standard deviation (RSD, %) of less than 2% for all the selected validation parameters. The estimated design space suggests the highest desirability (R2-0.998) at 60% of buffer in the mobile phase, pH 4.25, and flow rate of 0.7 mL/min. CONCLUSIONS: The QbD approach was used to design and develop the method by understanding the interaction between dependent and independent variables to get the optimum values. The developed method was validated successfully and can be useful for formulation scientists to estimate drug concentration and drug release profiles from complex nanoformulations. HIGHLIGHTS: The analytical approach was designed and quantified using a quality-by-design approach to make the RP-HPLC method more robust and efficient for the estimation of analytes from complex nanoformulations. The method is also useful to eliminate the interfering molecule during estimation by employing co-processing steps. The developed method saves time and cost of solvent and employs QbD as a requirement of recent regulatory concern.
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Gefitinibe , Comprimidos , Cromatografia Líquida de Alta Pressão/métodos , Gefitinibe/análise , Gefitinibe/química , Antineoplásicos/análise , Antineoplásicos/química , Nanopartículas/química , Composição de Medicamentos/métodos , Concentração de Íons de Hidrogênio , Cromatografia de Fase Reversa/métodosRESUMO
Ultraviolet (UV) radiation is a major contributor to skin aging, cancer, and other detrimental health effects. Sunscreens containing FDA-approved UV filters, like avobenzone, offer protection but suffer from photodegradation and potential phototoxicity. Encapsulation, antioxidants, and photostabilizers are strategies employed to combat these drawbacks. Octocrylene, an organic UV filter, utilizes nanotechnology to enhance sun protection factor (SPF). This review examines recent literature on octocrylene-enriched sunscreens, exploring the interplay between environmental impact, nanotechnological advancements, and clinical trial insights. A critical focus is placed on the environmental consequences of sunscreen use, particularly the potential hazards UV filters pose to marine ecosystems. Research in the Mediterranean Sea suggests bacterial sensitivity to these filters, raising concerns about their integration into the food chain. This review aims to guide researchers in developing effective strategies for photostabilization of UV filters. By combining encapsulation, photostabilizers, and antioxidants, researchers can potentially reduce phototoxic effects and contribute to developing more environmentally friendly sunscreens.
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Protetores Solares , Raios Ultravioleta , Protetores Solares/química , Protetores Solares/toxicidade , Humanos , Acrilatos/química , Nanotecnologia , Antioxidantes/química , Fator de Proteção SolarRESUMO
Nanotechnology is an emerging applied science delivering crucial human interventions. Biogenic nanoparticles produced from natural sources have received attraction in recent times due to their positive attributes in both health and the environment. It is possible to produce nanoparticles using various microorganisms, plants, and marine sources. The bioreduction mechanism is generally employed for intra/extracellular synthesis of biogenic nanoparticles. Various biogenic sources have tremendous bioreduction potential, and capping agents impart stability. The obtained nanoparticles are typically characterized by conventional physical and chemical analysis techniques. Various process parameters, such as sources, ions, and temperature incubation periods, affect the production process. Unit operations such as filtration, purification, and drying play a role in the scale-up setup. Biogenic nanoparticles have extensive biomedical and healthcare applications. In this review, we summarized various sources, synthetic processes, and biomedical applications of metal nanoparticles produced by biogenic synthesis. We highlighted some of the patented inventions and their applications. The applications range from drug delivery to biosensing in various therapeutics and diagnostics. Although biogenic nanoparticles appear to be superior to their counterparts, the molecular mechanism degradation pathways, kinetics, and biodistribution are often missing in the published literature, and scientists should focus more on these aspects to move them from the bench side to clinics.
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Several developments and research methods are ongoing in drug technology and chemistry research to elicit effectiveness regarding the therapeutic activity of drugs along with photoprotection for their molecular integrity. The detrimental effect of UV light induces damaged cells and DNA, which leads to skin cancer and other phototoxic effects. The application of sunscreen shields to the skin is important, along with recommended UV filters. Avobenzone is widely used as a UVA filter for skin photoprotection in sunscreen formulations. However, keto-enol tautomerism propagates photodegradation into it, which further channelizes the phototoxic and photoirradiation effects, further limiting its use. Several approaches have been used to counter these issues, including encapsulation, antioxidants, photostabilizers, and quenchers. To seek the gold standard approach for photoprotection in photosensitive drugs, combinations of strategies have been implemented to identify effective and safe sunscreen agents. The stringent regulatory guidelines for sunscreen formulations, along with the availability of limited FDA-approved UV filters, have led many researchers to develop perfect photostabilization strategies for available photostable UV filters, such as avobenzone. From this perspective, the objective of the current review is to summarize the recent literature on drug delivery strategies implemented for the photostabilization of avobenzone that could be useful to frame industrially oriented potential strategies on a large scale to circumvent all possible photounstable issues of avobenzone.
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Sulfobutylether ß-cyclodextrin (SBE-ß-CD) is a polyanionic cyclic oligosaccharide that contains glucopyranose units forming a torus ring-like structure. SBE-ß-CD is gifted with many favorable properties viz. relatively high solubility (>50 folds compared to ß-CD), improved stability, and biocompatibility that praised SBE-ß-CD as a smart polymer for drug delivery applications. Commercially, SBE-ß-CD is popular by its brand name Captisol®. The present review discusses the structure, properties, and preparation methods of SBE-ß-CD-based inclusion complexes (ICs). Furthermore, we discuss here the preparation and applications of SBE-ß-CD ICs-based nanoparticulate drug delivery systems, which combines the merits of both, ICs (enhanced solubility) and nanoparticles (NPs, targeted therapy). Patents on and FDA-approved Captisol®-enabled products are tabulated in the benefit of readers. The toxicological aspects and current clinical status of SBE-ß-CD or SBE-ß-CD-based products are briefly explained in the present review. In our opinion, the present review would be a pathfinder to allow dissemination of information on SBE-ß-CD.
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Polímeros Responsivos a Estímulos , beta-Ciclodextrinas , Biopolímeros , Sistemas de Liberação de MedicamentosRESUMO
The research study reflects the development of novel voriconazole (VCZ) loaded nanoparticles (NPs) for prolonged delivery for the management of ocular diseases. The in situ ophthalmic gel was prepared by incorporating NPs into carboxymethyl chitosan (CMCh) and poloxamer. The central composite design was used to optimize the process for the preparation of nanoparticles by the o/w solvent evaporation method. The developed nanoparticles were evaluated for the encapsulation efficiency (89.6 ± 1.2%), particle size (219.3 ± 1.8 nm), polydispersity index (PDI, 0.1), zeta potential (- 21.1 ± 1.12 mV), saturation solubility, DSC study, and drug release. The etherification process grafts carboxyl surface functional groups, on chitosan, and was confirmed by FTIR and NMR studies. The developed CMCh-poloxamer based gelling system was found to be clear and transparent with gelation temperature varying from 33 to 40 °C. The nanoparticle-loaded gel containing CMCh demonstrated enhanced antifungal activity against Candida albicans. The optimized batch containing CMCh showed improved mucoadhesion by 2.86-fold compared to VCZ nanosuspension. The drug release was prolonged up to 8 h with an ex vivo study suggesting the enhanced permeation across goat cornea estimated via fluorescent microscope. The hen's egg chorioallantoic membrane study revealed that the formulation was non-irritant and tolerated by the chorioallantoic membrane. The present study concludes that the VCZ loaded nanoparticulate in situ ophthalmic gel using CMCh may act as a potential alternative for traditional eye drops.
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Quitosana , Nanopartículas , Animais , Feminino , Poloxâmero/química , Quitosana/química , Voriconazol , Galinhas , Nanopartículas/química , Géis/química , Tamanho da Partícula , Coloides , Portadores de Fármacos/químicaRESUMO
The surface drying process is an important technology in the pharmaceutical, biomedical, and food industries. The final stage of formulation development (i.e., the drying process) faces several challenges, and overall mastering depends on the end step. The advent of new emerging technologies paved the way for commercialization. Thin film freezing (TFF) is a new emerging freeze-drying technique available for various treatment modalities in drug delivery. TFF has now been used for the commercialization of pharmaceuticals, food, and biopharmaceutical products. The present review highlights the fundamentals of TFF along with modulated techniques used for drying pharmaceuticals and biopharmaceuticals. Furthermore, we have covered various therapeutic applications of TFF technology in the development of nanoformulations, dry powder for inhalations and vaccines. TFF holds promise in delivering therapeutics for lung diseases such as fungal infection, bacterial infection, lung dysfunction, and pneumonia.
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Recovery of lactose from the whey using sonocrystallization was studied experimentally. The effect of sonication medium and irradiation power levels was evaluated using three different ultrasonic equipments. Effects of various parameters such as sonication time, pH of the medium, antisolvent (acetone and acetone-ethanol mixture) and concentration of lactose were determined. The optimal parametric conditions were analyzed using differential scanning calorimetry, thermogravimetric analysis, particle size distribution, and zeta potential measurements. Overall, the highest lactose recovery was obtained using a mixture of acetone and ethanol as antisolvent in bath sonication as well as atomization process.
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Drug delivery to lungs via pulmonary administration offers potential for the development of new drug delivery systems. Here we fabricated the etofylline (ETO) encapsulated mannose-anchored N,N,N-trimethyl chitosan nanoparticles (Mn-TMC NPs). The prominent characteristics like biocompatibility, controlled release, targeted delivery, high penetrability, enhanced physical stability, and scalability mark Mn-TMC NPs as a viable alternative to various nanoplatform technologies for effective drug delivery. Mannosylation of TMC NPs leads to the evolution of new drug delivery vehicle with gratifying characteristics, and potential benefits in efficient drug therapy. It is widely accepted that following pulmonary administration, the introduction of mannose to the surface of drug nanocarriers provide selective macrophage targeting via receptor-mediated endocytosis. The fabricated Mn-TMC NPs exhibited particle size of 223.3 nm, PDI 0.490, and ζ-potential -19.1 mV, drug-loading capacity 76.26 ± 1.2%, and encapsulation efficiency of 91.75 ± 0.88%. Sustained drug release, biodegradation studies, stability, safety, and aerodynamic behavior revealed the effectiveness of prepared nanoformulation for pulmonary administration. In addition, the in vivo pharmacokinetic studies in Wistar rat model revealed a significant improvement in therapeutic efficacy of ETO, illustrating mannosylation a promising approach for efficient therapy of airway diseases following pulmonary administration.
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Quitosana , Portadores de Fármacos , Pneumopatias/tratamento farmacológico , Manose , Nanopartículas , Teofilina/análogos & derivados , Animais , Quitosana/química , Quitosana/farmacocinética , Quitosana/farmacologia , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Portadores de Fármacos/farmacologia , Pneumopatias/metabolismo , Pneumopatias/patologia , Masculino , Manose/química , Manose/farmacocinética , Nanopartículas/química , Nanopartículas/uso terapêutico , Ratos , Ratos Wistar , Teofilina/química , Teofilina/farmacocinética , Teofilina/farmacologiaRESUMO
The aim of this work was to evaluate the in vitro performance of nebulized nanosuspension formulation when nebulized using ultrasonic nebulizer. The present investigation deals with successful formulation of Beclomethasone dipropionate loaded HPMCP nanospheres prepared by solvent evaporation technique using PEG 400 as a stabilizer. Beclomethasone dipropionate is a water insoluble drug molecule was encapsulated in HPMCP nanospheres to have pH dependent solubility at basic pH for targeted drug delivery in lung and studied for in vitro cytotoxicity and immediate release capability. The synthesized nanospheres were characterized through drug excipient compatibility, surface topography; mean particle size , zeta potential, PDI, entrapment efficiency and drug loading, in vitro diffusion, aerodynamic, in vitro cytotoxicity and stability studies. The mean particle size and PDI of the optimized batch (F1) had 197.6±0.40 nm and 0.324 ±0.35, respectively. The % entrapment efficiency and % drug loading was found to be 86.56±1.32 and 8.30±0.27, respectively. The optimized batch F1 showed % cumulative drug release 94.77±0.24 at 1 h. The formulation showed cell viability up to 91.28%. It can be concluded that, Beclomethasone dipropionate loaded HPMCP nanospheres was found to be safe, stable with significant increase in solubility and bypass the liver.