Development and validation of HPLC method for determination of benidipine hydrochloride in lipid vesicles formulations

In the current study, a novel high-performance liquid chromatographic method is being developed and validated to estimate benidipine hydrochloride in lipid-based pharmaceutical formulations including transfersome, ethosome, and transethosome. The chromatographic separation was accomplished on a ZORBAX Eclipse Plus C18 (4.6mm x 150mm) analytical column with a mobile phase consisting of a mixture of methanol and 50 mM phosphate buffer solution at a ratio of 70:30 (v/v). A standard calibration curve was used to quantitatively determine the medication at a UV wavelength of 237 nm. The limit of detection (LOD) and limit of quantitation (LOQ) were determined to be 0.005µg/ml and 0.015µg/ml, respectively. The relative standard deviation (%RSD) of the intra-day and inter-day studies for benidipine hydrochloride was less than 2%, and the percentage recovery of benidipine hydrochloride was found to be in the range of 98.57-100.27%. The method is specific, linear, accurate, precise, robust, and sensitive for its intended purpose, according to the results of the method validation. To determine the amount of benidipine hydrochloride and the effectiveness of drug entrapment in lipid-based formulated membrane like cell structures namely Transfersomes, Ethosomes, and Transethosomes the current method was successfully applied

A new and rapid UV-Visible spectrophotometric method for benidipine hydrochloride determination: Development and validation

A simple, sensitive and specific ultraviolet spectrophotometric method has been established for the determination of benidipine hydrochloride. The wavelength of maximum absorbance (λmax) for benidipine was found to be 237 nm. Linearity of this method was observed in a range of 2.0 – 16.0 μg/mL. The method showed high sensitivity with good reproducibility of results. The limit of detection and the limit of quantification were 0.34 and 1.02 μg/mL, respectively. The calibration curve was constructed by plotting a graph of the absorbance versus concentration. The coefficient of correlation was higher than 0.99. The regression equation of this curve is y = 0.0544x – 0.0526. The percentage of drug recovery was found in the acceptable range (99.72 – 101.66%), and the coefficient of variation for the precision of this method was found to be less than 2.0. The proposed method can be suitable for the analysis of benidipine in tablet formulations for quality control purposes

Stability of paracetamol instant jelly for reconstitution: Impact of packaging, temperature and humidity

The stability of the medicinal product is a major concern in the pharmaceutical industry and health authorities, whose goal is to guarantee that drugs are delivered to patients without loss of therapeutic properties. This study aims to evaluate the effect of environmental conditions and packaging on the stability of paracetamol instant jelly sachets based on both chemical and physical stability. The paracetamol instant jelly was packaged in plastic sachets (packaging 1) and sealed aluminium bags in screw-capped amber glass bottles (packaging 2), which were stored in real-time and accelerated stability chambers for 3 months. Samples were taken out from the chambers and were characterised for appearance, moisture content, texture, viscosity, in vitro drug release, paracetamol content, and 4-aminophenol level at different time points. The real-time storage condition at a lower temperature maintained the stability of the paracetamol instant jelly, while the accelerated condition led to a significant change in the formulation properties. In addition, the proper packaging of paracetamol instant jelly maintained the paracetamol’s stability, regardless of environmental conditions, for three months. The results show that the environmental conditions and packaging play a significant role in maintaining paracetamol instant jelly stability

A review on taste masked multiparticulate dosage forms for paediatric for tenacity and toughness improvement

Taste refers to those sensations perceived through taste buds on the tongue and oral cavity. The unpleasant taste of drugs leads to the refusal of taking the medicine in the paediatric population. It is widely known that a pharmaceutical product's general acceptability is the result of numerous contributing components such as swallowability, palatability (taste, flavour, texture, and mouthfeel), appearance, ease of administration, and patient characteristics. Multiparticulate as a dosage form is a platform technology for overcoming paediatrics' incapacity to swallow monolithic dosage forms, masking many medications' inherent nasty taste, and overcoming the obstacles of manufacturing a commercially taste masked dosage form. This review will discuss the considerations that must be taken into account to prepare taste masked multiparticulate dosage forms in the best way for paediatric use

Ibuprofen-loaded chitosan–lipid nanoconjugate hydrogel with gum arabic: Green synthesis, characterisation, in vitro kinetics mechanistic release study and PGE2 production test

Ibuprofen is a well-known non-steroidal anti-inflammatory (NSAID) medicine that is often used to treat inflammation in general. When given orally, it produces gastrointestinal issues which lead to lower patient compliance. Ibuprofen transdermal administration improves both patient compliance and the efficacy of the drug. Nanoconjugation hydrogels were proposed as a controlled transdermal delivery tool for ibuprofen. Six formulations were prepared using different compositions including chitosan, lipids, gum arabic, and polyvinyl alcohol, through ionic interaction, maturation, and freeze–thaw methods. The formulations were characterised by size, drug conjugation efficiency, differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR). Further analysis of optimised hydrogels was performed, including X-ray diffraction (XRD), rheology, gel fraction and swelling ability, in vitro drug release, and in vitro macrophage prostaglandin E2 (PGE2 ) production testing. The effects of ibuprofen’s electrostatic interaction with a lipid or polymer on the physicochemical and dissolution characterisation of ibuprofen hydrogels were evaluated. The results showed that the S3 (with lipid conjugation) hydrogel provided higher conjugation efficiency and prolonged drug release compared with the S6 hydrogel

A bioanalytical method for quantification of telmisartan in rat plasma; development, validation and application to pharmacokinetic study

The telmisartan was determined in a rat plasma using developed and validated a reversed-phase high performance liquid chromatographic (HPLC). The pre-treatment of the plasma sample involving liquid-liquid extraction using ethanol as the extracting solvent. The HPLC method validation has been shown a linear calibration curve over a plasma concentrations range of 0.7 to 10µg/mL with a correlation coefficient of 0.9979, the limit of detection and the limit of quantification were determined to be 0.025µg/ml and 0.07µg/ml, respectively. The precision and accuracy were in an acceptable limit. The pharmacokinetic parameters of telmisartan were adequately evaluated following a single oral dose (4mg/kg) in Sprague-Dawley rats. The results observed conclude that the developed bioanalytical HPLC method is appropriate and applicable as an analytical tool in the pharmacokinetic study of telmisartan

Micro and nano-carriers-based pulmonary drug delivery system: Their current updates, challenges, and limitations – A review

The lung is an attractive target for drug delivery because of the ease of non-invasive administration via inhalation, bypassing metabolism in the liver, direct delivery to the respiratory system for treatment of respiratory diseases, and a large surface area for drug absorption. Nanocarrier systems offer several benefits for pulmonary drug delivery, including uniform drug distribution among alveoli, improved drug solubility, sustained drug release, which reduces the dosing frequency and enhances patient compliance, and potential for cell drug internalization. Nanomedicine is also being utilized to combat emerging infectious illnesses like SARS-CoV, SARS-CoV-2, MERS-CoV, and influenza A/H1N1. This review gives a quick rundown of pulmonary diseases caused by infectious agents such as bacterial, viral, and biological roadblocks that prevent effective treatment of recalcitrant respiratory tract infections. We emphasized and summarized recent efforts to combat these infections using novel inhaled formulation-mediated pulmonary delivery strategies like nanocarriers such as liposomes, polymeric nanoparticles, and SLNs. In addition, we also reviewed the latest findings and advancements regarding the development of inhalable novel formulations that circumvent biological barriers and boost drug bioavailability

Development and Validation of HPLC Method for Determination of Benidipine Hydrochloride in Lipid Vesicles Formulations

Abstract: In the current study, a novel high-performance liquid chromatographic method is being developed and validated to estimate benidipine hydrochloride in lipid-based pharmaceutical formulations including transfersome, ethosome, and transethosome. The chromatographic separation was accomplished on a ZORBAX Eclipse Plus C18 (4.6mm x 150mm) analytical column with a mobile phase consisting of a mixture of methanol and 50 mM phosphate buffer solution at a ratio of 70:30 (v/v). A standard calibration curve was used to quantitatively determine the medication at a UV wavelength of 237 nm. The limit of detection (LOD) and limit of quantitation (LOQ) were determined to be 0.005µg/ml and 0.015µg/ml, respectively. The relative standard deviation (%RSD) of the intra-day and inter-day studies for benidipine hydrochloride was less than 2%, and the percentage recovery of benidipine hydrochloride was found to be in the range of 98.57-100.27%. The method is specific, linear, accurate, precise, robust, and sensitive for its intended purpose, according to the results of the method validation. To determine the amount of benidipine hydrochloride and the effectiveness of drug entrapment in lipid-based formulated membrane like cell structures namely Transfersomes, Ethosomes, and Transethosomes the current method was successfully applied. Keywords: Benidipine hydrochloride, HPLC, Lipid vesicles, Entrapment efficiency, Drug content

Rheology profiles of gelling agents for food and pharmaceutical applications

Rheology of gelling agents is important for the formulator in both food and pharmaceutical industry. In pharmaceutical industry, gelling agent s are widely used in liquid preparations, semisolid preparations and even in solid formulations. They are used to increase the viscosity, stabilise the formulation and control drug release. Most of these uses stem from the rheological properties of the gelling agent. The idea of this work came after we tried to formulate a semisolid formulations, topical and for oral use. We tried to find the rheological profiles of different gelling polymer in order to choose the one that best fits our need. However, we found lack in the data available in the literature. Thus, the best way was to screen wide range of gelling agents and study their rheology in some details. After that, each formulator can choose the one that suits the application. This work describes the rheological profiles of different gelling agents without discussing their suitability for specific application. The reason is that each application needs different properties. We hope that the data presented here give good guidance to the formulator to choose the suitable gelling agent for the intended formulatio

Liposomes or Extracellular Vesicles: A Comprehensive Comparison of Both Lipid Bilayer Vesicles for Pulmonary Drug Delivery

The rapid and non-invasive pulmonary drug delivery (PDD) has attracted great attention compared to the other routes. However, nanoparticle platforms, like liposomes (LPs) and extracellular vesicles (EVs), require extensive reformulation to suit the requirements of PDD. LPs are artificial vesicles composed of lipid bilayers capable of encapsulating hydrophilic and hydrophobic substances, whereas EVs are natural vesicles secreted by cells. Additionally, novel LPs-EVs hybrid vesicles may confer the best of both. The preparation methods of EVs are distinguished from LPs since they rely mainly on extraction and purification, whereas the LPs are synthesized from their basic ingredients. Similarly, drug loading methods into/onto EVs are distinguished whereby they are cell- or non-cell-based, whereas LPs are loaded via passive or active approaches. This review discusses the progress in LPs and EVs as well as hybrid vesicles with a special focus on PDD. It also provides a perspective comparison between LPs and EVs from various aspects (composition, preparation/extraction, drug loading, and large-scale manufacturing) as well as the future prospects for inhaled therapeutics. In addition, it discusses the challenges that may be encountered in scaling up the production and presents our view regarding the clinical translation of the laboratory findings into commercial products