Drug Content Research Articles

Analytical Method Validation and Simultaneous Determination of Ketotifen Fumarate and Cyproheptadine Hydrochloride in Divided Powder by RP-HPLC Method

Ketotifen fumarate and cyproheptadine HCl are the most popular prescription for children at “X” hospital in Yogyakarta. The interest for studying this divided powder was related to the stability test towards human health. Hence, it was important to developed a validated analytical method to quantify content of active drug from sample. In this study, a reversed phase HPLC (RP-HPLC) method was validated and applied for determining content of ketotifen fumarate and cyproheptadine hydrochloride in divided powder. The developed RP-HPLC method was met the requirement of selectivity and sensitivity. Calibration curve formulas of ketotifen fumarate and cyproheptadine hydrochloride were y = 27714x-79111 (r=0.9945) and y = 26324x+72581 (r=0.9935) in the range of 10.9-54.5 and 10.6-53.0 µg/mL, respectively. Accuracy and intermediate precision were assessed on both standard solution and samples spiked with standard solution of ketotifen fumarate and cyproheptadine hydrochloride. It was found that both standard solution and the spiked samples solution were met the requirement of recovery of 80-110% and RSD of less than 7.3% for intraday and interday analysis. Content of ketotifen fumarate and cyproheptadine hydrochloride in sample (n=7) were 16.574±0.098 and 30.640±0.035 µg/mL, respectively. It can be concluded that the RP-HPLC method was successfully validated and applied in the determination of ketotifen fumarate and cyproheptadine hydrochloride in divided powder.

Formulation and Optimization of Fast Dissolving Tablets of Zidovudine.

Fast-dissolving tablets (FDTs) have emerged as a prominent alternative to conventional oral dosage forms, particularly for drugs requiring rapid onset of action. This study aims to formulate and optimize fast-dissolving tablets of zidovudine, an antiretroviral medication used in the treatment of HIV/AIDS. The primary objective was to enhance patient compliance by ensuring the tablet disintegrates and dissolves quickly in the oral cavity without the need for water. Using various superdisintegrants like sodium starch glycolate and cross-carmellose sodium into, multiple formulations were prepared. The optimized formulation was evaluated based on pre-compression and post-compression parameters, including hardness, friability, disintegration time, dissolution profile, and drug content uniformity. The study found that the incorporation of superdisintegrants significantly improved the dissolution rate of zidovudine, thus offering a promising approach for patients with swallowing difficulties and ensuring better therapeutic efficacy.

Development and Characterization of Oxiconazole Loaded Plga Nanogel.

The goal of the current study is to develop and improve polylactic co-glycolic acid (PLGA) loaded with oxiconazole nanogel for topical application. Oxiconazole Nanoprecipitation was used to create the nanoparticles method using PLGA and acetone. The point prediction method served as the foundation for the ideal oxiconazole nanoparticle composition using the Minitab®21 software, three levels two factors (32 ). The optimized composition of oxiconazole nanoparticle showed a particle size of 185 ± 0.5nm with an entrapment efficiency of 95.2 ± 0.09%. Using chitosan, a naturally occurring polymer, the ideal oxiconazole nanoparticle composition was further transformed into a gel formulation. The developed topical nano gel formulation underwent additional evaluations for antifungal, drug release, permeability, and nano gel characterization. The developed oxiconazole nanogel formulation had the ideal drug content, pH, viscosity, and spreadability. The results of the medication release and penetration investigation showed that Oxiconazole released slowly (74.06 ± 0.5%) with significantly enhanced permeation across Franz diffusion cell using membrane. The antifungal ex-vivo study and skin irritancy study of nanogel results would conclude higher activity of oxiconazole nano gel. According to the overall analysis of the data, oxiconazole nanogel is the best delivery method for treating fungal infections on the skin.

Nanosponges as a Drug Delivery System: Methods, Characteristics and Applications

Nanosponges, which are crosslinked polymer nanometers in sized used for drug transport, have a unique three-dimensional appearance. Their versatility lies in their ability to accommodate drugs of various sizes. The research approach, polymer type, and drug content determine the diversity of nanosponges. Nanosponges excel as delivery systems due to their capacity for controlled and targeted drug release. They offer the flexibility to regulate the duration of drug action and residence time. Their biodegradable composition ensures low toxicity and safe usage. Available voids, along with the size of the test molecule, play a crucial role in the efficiency of encapsulation. Nanosponges exhibit numerous applications such as cancer treatment, transportation of enzymes and biocatalysts, oxygen, modification of drug solubility, and immobilization of enzymes. This study emphasizes the preparation method, characterization, influencing factors, drug loading, recent advancements, and patents in the field of nanosponges.

A Nondestructive and Rapid Method for the Determination of Triamterene Content by Transmission Raman Spectroscopy Combined with Chemometrics

Background: Triamterene is a potassium-conserving diuretic mainly used in the treatment of edematous diseases. Although there are some methods to measure the content of triamterene, the existing methods have the characteristics of sample destructiveness and low flux, making it difficult to meet the needs of online monitoring. In recent years, transmission Raman spectroscopy (TRS), as a new technology for the determination of drug content, has emerged as being nondestructive and rapid and provides a new method for the determination of triamterene content. Objective: In this study, we used transmission Raman spectroscopy combined with partial least squares (PLS) approaches to establish a six concentration levels model for measuring the content of triamterene. The model was applied to determine whether tablets are commercially available. Method: Firstly, TRS was used to collect the spectra of the principal components and mixed excipients of triamterene, and the feasibility test was carried out. Secondly, six concentration levels were determined by the design of experimental (DOE), and hand-made tablets were prepared to obtain corresponding spectra. The content prediction model was established by the PLS method, and the content of triamterene was determined by high-performance liquid chromatography (HPLC) to correct the model. Finally, the model was applied to the determination of triamterene in commercially available tablets. Results: The results showed that the established model was successfully applied to the determination of triamterene. The values of RMSEC (0.0089783) and RMSECV (0.0097241) of the final model were very low and close to each other. The relative error of 12 hand-made tablets predicted by this model was less than 5% compared with the results determined by HPLC. In addition, in the process of applying the model to the determination of the content of commercially available tablets, the accuracy of the model can be significantly improved by adding the spectrum of commercially available tablets. The corrected model was used to determine the content of triamterene in two commercially available tablets. The results showed that the relative error was less than 5%. Conclusion: We described a new strategy to analyze the content of active pharmaceutical ingredients (API) in triamterene tablets by TRS with PLS. The established model has the advantage of non-destructive and rapid quantitation, which can provide a new method for real-time monitoring of production lines and promote the development of process analytical technology (PAT).

Development and Characterization of Olaparib-Loaded Solid Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) for Pharmaceutical Applications.

This study aims to enhance the solubility of Olaparib, classified as biopharmaceutical classification system (BCS) class IV due to its low solubility and bioavailability using a solid self-nanoemulsifying drug delivery system (S-SNEDDS). For this purpose, SNEDDS formulations were created using Capmul MCM as the oil, Tween 80 as the surfactant, and PEG 400 as the co-surfactant. The SNEDDS formulation containing olaparib (OLS-352), selected as the optimal formulation, showed a mean droplet size of 87.0 ± 0.4 nm and drug content of 5.53 ± 0.09%. OLS-352 also demonstrated anticancer activity against commonly studied ovarian (SK-OV-3) and breast (MCF-7) cancer cell lines. Aerosil® 200 and polyvinylpyrrolidone (PVP) K30 were selected as solid carriers, and S-SNEDDS formulations were prepared using the spray drying method. The drug concentration in S-SNEDDS showed no significant changes (98.4 ± 0.30%, 25℃) with temperature fluctuations during the 4-week period, demonstrating improved storage stability compared to liquid SNEDDS (L-SNEDDS). Dissolution tests under simulated gastric and intestinal conditions revealed enhanced drug release profiles compared to those of the raw drug. Additionally, the S-SNEDDS formulation showed a fourfold greater absorption in the Caco-2 assay than the raw drug, suggesting that S-SNEDDS could improve the oral bioavailability of poorly soluble drugs like olaparib, thus enhancing therapeutic outcomes. Furthermore, this study holds significance in crafting a potent and cost-effective pharmaceutical formulation tailored for the oral delivery of poorly soluble drugs.

Design and in vitro Evaluation of Cocoa Butter-based Amlodipine Besylate Fast Melt Tablets

Background: Oral fast-melting tablets (FMTs) have been gaining popularity due to their advantages in resolving swallowing issues of conventional oral tablets. Cocoa butter is an excipient of choice to develop FMT with an acceptable taste and faster onset of action of the drug. Purpose: The present study aimed to prepare and characterize the amlodipine besylate-loaded cocoa butter FMTs. objective: To prepare and characterise the formulation of cocoa butter tablet as fast melt buccal delivery system of amlodipine besylate. Method: Amlodipine besylate FMTs were prepared using a simple freezing (refrigeration) method. Cocoa butter (Form V) was used as the base to achieve a final tablet weight of 500 mg with drug and other functional excipients. The designed prototype tablet formulations were subjected to disintegration tests to determine the robust selected batch. The formulation F4, containing 7% high-molecular-weight chitosan, exhibited the quickest disintegration time of 1.45 ± 0.10 min. Afterwards, the selected formulation, F4, was subjected to quality evaluation parameters. Results: Fourier transform infrared spectroscopy (FTIR) studies revealed that there was no incompatibility between amlodipine besylate, cocoa butter, and other excipients. The average hardness of the F4 formulation tablet batch was found to be 2.69 ± 0.21 kg/cm2 and a friability of less than 1%. The drug content in F4 tablets was found to be 102.38 ± 5.29% and showed an in-vitro drug release of 94.30 ± 2.63% within 30 min. Over a six-month stability testing period, the chosen F4 formulation did not significantly change in terms of tablet average weight, disintegration time, drug content, and in-vitro dissolution rate. Conclusions: Selected formulation F4 with 7% of high molecular weight chitosan exhibited good physical properties, indicating the suitability of cocoa butter as a base to produce FMTs with the aid of a natural super-disintegrant.

In vitro and in vivo evaluation of in situ forming polyester implants for the extended release of carvedilol.

Polyester based in situ forming implants (ISFIs) are injectable long-acting drug delivery systems that offer a wide range of unique advantages. As a result of these advantages, two relatively highmolecular weight, ester terminated grades of poly (D,L-lactide-co-glycolide) (PLGA) and poly(D,L-lactide) (PLA) were evaluated for their ability (i) to form ISFIs loaded with carvedilol, and (ii) to control its release both in vitro and in vivo. At a polymeric concentration of 40% w/w, implant solutions were syringeable, injectable, and able to encapsulate carvedilol to a high degree (encapsulated drug% > 97%). When visualized using scanning electron microscopy (SEM), implants were found to have a dense thin surface atop porous sublayers. As for their in vitro evaluation, PLGA and PLA implants were able to maintain drug release over the course of 49 and 84 days, respectively. On the other hand, in vivo drug release from both implants was almost identical and lasted for only 42 days. This may be due to the overriding effect of the similar host environment at the injection site that diminished the effect of polymeric physiochemistry on phase inversion and drug release. Lastly, while the polymer-free drug/NMP solution completely released its drug content within the initial half hour in vitro, the formulation extended drug release in vivo. This could be due to a yet to be investigated interaction between carvedilol and NMP under in vivo conditions. These results cement the significance of formulating carvedilol loaded ISFIs for the management of chronic conditions.

Preparation and Evaluation of Itraconazole Nanoparticle Lipid Carrier Gel for Dermatophytosis

Fungal infection is one of the common dermatological diseases. Drug delivery systems for topical use have shown significant advantages in targeting the drug to the action site in the body and also reduces the systemic side effects. Itraconazole was chosen as a model drug with low aqueous solubility. In the present study an attempt was made to prepare itraconazole loaded nanostructured lipid carrier (NLC). Different formulations were prepared by hot homogenization technique using solid lipid and liquid lipid (Compritol 888 & Caprol PGE 860) and surfactants (Poloxamer 188, tween 80). All the Formulations were characterized for drug content, entrapment efficiency, particle size, poly dispersity index, zeta potential &in vitro drug release and FTIR was done to study any interaction between excipients. The best formulation shows better drug release and entrapment efficiency 83.2%. the best formulation F3 showed better in-vitro drug release 55.46% at the end of 8th hour. The F3 was made into gel using Carbopol as a gelling agent. SEM study revealed that the NLC gel shows the particle size was found to be 500 nm in size smooth surfaces. NLC gel shows Drug release of NLC gel followed non- Fickian diffusion. NLC gel were stable at 40 ± 2ֹ°C and 75 ± 5% RH. Thus, the prepared NLC gel proved to be a potential candidate as a topical nanoparticulate sustained drug delivery system for itraconazole (BCS class II drug). keywords: Itraconazole, Nanoparticle Lipid Carrier, Lipids.

Formulation and evaluation of medicated lozenges containing the solid dispersion of Clotrimazole /PEG 6000 for the treatment of oral candidiasis

The study aimed to formulate Clotrimazole (CLM) as solid dispersion medicated lozenges with enhanced dissolution for treating oropharyngeal candidiasis. They are suitable for many patients and easy to administer. The study used the solvent evaporation method to prepare solid dispersions of CLM using polyethylene glycol 6000 and polyvinyl pyrrolidone at different drug-to-carrier weight ratios. The study found that PEG 6000, when used at a 1:1 weight ratio, significantly improved the dissolution of CLM. The results of the FTIR studies showed that the drug was dispersed within PEG 6000, and there was no drug interaction with the excipients used in medicated lozenge formulations. A 32-factorial design was used to develop, optimize, and evaluate nine formulations of the solid dispersion of CLM/PEG 6000 medicated lozenges for improved therapeutic outcomes. We fabricated the lozenges using biocompatible polymeric gelling agents (chitosan, methyl cellulose, and sodium alginate) at three different levels (0.5, 1, and 1.5%). All the medicated lozenges were uniform in weight and drug content within USP limits, with complete drug release rates ranging from 10–20 minutes for chitosan and sodium alginate formulations, compared to 60 minutes for methyl cellulose. The results showed that the type of polymer and its concentration significantly impacted drug release. The optimized formulation, F-3, containing 1.5% CH, exhibited a drug release of 100.83% ±0.68 at the end of 10 minutes. It demonstrated significant antifungal activity against Candida albicans (p < 0.05), making it suitable for drug delivery in the oral cavity.

Formulation and Comparison of Herbal Gels Containing Essential oils and their Antimicrobial Evaluation.

The current study aimed to formulate and evaluate herbal gels con-taining essential oils for the treatment of infection caused by microbial species, i.e., S. au-reus, E. coli, P. aeruginosa, and B. subtilis. These species are also responsible for acne directly and indirectly. The gels were prepared using a gelling agent with 1% Carbopol-940, and they were further evaluated for physical appearance, drug content, in-vitro drug release, viscosity, extrudability, pH, and spreadability. Further, anti-microbial screening was done with various microbial species. Studies revealed that the gel was highly effective against the selected species ex-cept for the fungal strain. ZOI was observed ranging from 3.1 ± 0.01 mm to 13.4 ± 0.14 mm. The maximum ZOI was observed at 13.4 ± 0.14 mm against S. aureus. The physical properties of the gel satisfied the standard parameters. The prepared herbal gel was found to have highly promising activity against bacterial species associated with bacterial infection but in a dose-dependent manner. How-ever, more research is required.

Formulation and <i>in vitro</i> Evaluation of Liquisolid Compact of Celecoxib

<i>Introduction</i>: The liquisolid technique presents a promising avenue for enhancing the dissolution rate and bioavailability of poorly water-soluble drugs like celecoxib. This study investigated the formulation and evaluation of celecoxib tablets using this technique. <i>Aim</i>: To formulate and evaluate celecoxib tablets using the liquisolid technique, with the objective of enhancing its dissolution rate and bioavailability. <i>Methods</i>: Celecoxib tablets were prepared using the liquid-solid technique by incorporating a non-volatile liquid medication carrier and a suitable solid carrier. Various formulations were developed by altering the ratios of drug, carrier, and coating materials. The prepared tablets were characterized for their physical properties, drug content uniformity, <i>in vitro</i> dissolution behavior, and compatibility using Fourier-transform infrared (FTIR) spectroscopy. <i>Results</i>: The solubility profile showed that the maximum rate of solubility was recorded in PEG-400 (11.03 ± 0.01) when compared to other non-volatile solvents. The angle of slide, indicated that the excipients used were within the acceptable limit of 33°. The FTIR spectroscopy showed compatibility of the drug and excipients. The results of the SEM showed that spherically-shaped vesicles were formed. Evaluation of the pre-compression parameters indicated that the drug content was highest in batch F-11 hence its optimization (96.1 ± 0.90). The post compression evaluation indicated that the official tests were within the acceptable range for disintegration time (2.25 ± 0.35). The results of the <i>in vitro</i> release studies of the optimized formulation, conventional tablet and reference commercial tablet showed that the amount of drug released increased steadily with time over the 1-hour period. <i>Conclusion</i>: Our findings underscore its viability as a strategy to enhance the therapeutic efficacy of poorly water-soluble drugs, offering promising prospects for pharmaceutical formulation.

Formulation and Evaluation of Solid Dispersion of Phenytoin by Solvent Evaporation Technique

The aim of the present study is Formulation and Evaluation of Phenytoin by making solid dispersion with polyvinyl alcohol and inclusion complexation with HPβ Cyclodextrin, β Cyclodextrin. Solid dispersion of Phenytoin is prepared with Solvent Evaporation method. Phenytoin belongs to BCS class II drug which is characterized by high membrane permeability, slow dissolution rate due to low aqueous solubility. It is an anti-epileptic or anti- convulsant is used to treat wide variety of Seizures. The Phenytoin solid dispersions were prepared by solvent evaporation method at 1:0.25, 1:0.5, 1:0.75, 1:1, 1:1.25, 1:1.5 ratios of Phenytoin to HP β CD, β CD and PVA. The prepared dispersions were evaluated by solubility studies, in-vitro dissolution studies, melting point determination, drug content uniformity, entrapment efficiency and FT-IR studies. Finally comparing all the formulations (P:HPβ F1-P:HPβ F6) (P: βF1-P βF6) and (P:PF1-P:PF6) formulation P:PF4 containing Phenytoin: Polyvinyl alcohol (1:1) shows better result at the end of 90 min with drug release 93.99%, hence it was selected as the best formulation. By release kinetic studies of best formulation of Phenytoin with zero order and first order we can say that the best formulation follows first order kinetics studies having r2 value 0.945 where as zero order release kinetics studies having r2 value 0.849. The results indicated as formulated solid dispersion tablets displayed better dissolution profiles as compared to existing commercial tablets.

A novel mucoadhesive film containing probiotic extract for oral candidiasis treatment: Formulation and antifungal evaluation

Probiotic strains offer a novel and potentially effective approach to treat oral candidiasis. Buccal mucoadhesive films have attracted considerable attention in recent years due to their unique ability to adhere and persist on the oral mucosa, while gradually releasing their encapsulated drug content. Therefore, the aim of the study was to develop mucoadhesive films containing probiotic extract for treatment of oral candidiasis. Mucoadhesive films were fabricated with hydrophilic polymers, such as polyvinyl alcohol (PVA) and hydroxy propyl methyl cellulose (HPMC). Then, films were evaluated regarding their thickness, pH, tensile strength and elongation, swelling, in vitro release and antifungal activity. The type of polymer used had an impact on the mechanical properties, swelling and release of the films. Films prepared using PVA showed significantly higher tensile strength and elongation at break values compared to those prepared using HPMC. However, swelling index increased with enhancing HPMC concentration in the films. The release of probiotic extract from the film prepared with HPMC occurred slowly. Based on these results, films containing 54 % HPMC and 26 % PVA were selected as optimal formulation. Moreover, it was found that optimal film containing probiotic extract could inhibit the growth of Candida albicans. Regarding to the obtained results, probiotic oral adhesive mucoadhesive films can be considered as a promising alternative to traditional methods in the treatment of candidiasis.

Preparation and In Vitro Evaluation of Montelukast Sodium-Loaded 3D Printed Orodispersible Films for the Treatment of Asthma.

This research aims to produce orodispersible films (ODFs) and determine their potential use in the oral delivery of montelukast sodium for asthma treatment and allergic rhinitis. ODFs were successfully developed by Three-dimensional (3D) printing using propylene glycol (PG), and hydroxypropyl methylcellulose (HPMC), polyethylene glycol 400 (PEG). Finally, the amount of montelukast sodium in the ODFs was 5% (w/w). Drug-excipients compatibility with Fourier Transformed Infrared (FTIR) spectroscopy, mass uniformity, thickness, disintegration time, folding endurance, moisture absorption, pH, in vitro drug release (dissolution), drug content, moisture loss, moisture content, mechanical properties, and cytotoxicity studies were performed on the prepared films. All formulations disintegrated in approximately 40 s. Over 98% of drug release from all films within 2 min was confirmed. It was reported that Fm1-4 (8% HPMC and 1% PEG) and Fm2-4 (10% HPMC and 3% PEG) are more suitable for drug content, but Fm2-4 may be the ideal formulation considering its durability and transportability properties. Based on the characterization results and in vitro release values, the montelukast sodium ODF can be an option for other dosage forms. It was concluded that the formulations did not show toxic potential by in vitro cytotoxicity study with 3T3 cells. This new formulation can efficiently treat allergic rhinitis and asthma diseases.

Effect of Pluronic F127 Concentration on Gelling Temperature and other Parameters of Lomustine Mucoadhesive In-Situ Gel

Pluronic F127 is one of the widely used thermoreversible gelling agent, and used in sol-to-gel transformation. It has been used to localize drug delivery such as nose-to-brain delivery which allows the direct targeting of drug molecules bypassing the systemic effect and BBB (Blood Brain Barrier). The anticancer drug lomustine had poor oral bioavailability in addition to its serious side effect, therefore, developing more effective drug delivery with direct targeting towards the brain through intra-nasal administration applying nanoemulsion-based-in situ gel technology is a promising alternative. The work involved formulation of lomustine as in situ gel using Pluronic F127 and study the effect of the polymer on solution to gel transition temperature, gelation behaviour, spreadability, mucoadhesive force, residence time and residence drug percentage, as well as in vitro drug release. The results showed acceptable pH and high drug content, beside increased Pluronic percentage (from 15 to 20%) led to reduced gelation temperature from 33°C to 27°C and spreadability, improved gelling properties from + to +++, increasing mucoadhesive force from 4965.33 to 9866.30 dyne/cm2 as well as prolonged residence time from 30 to 66 min and in vitro drug release where was 120 min for 100% drug release from F1 that contained 15% of the polymer to 210 min for F3 with 20% polymer. Therefore, modifying the Pluronic F127 percent in the in situ formulas could optimize the required formula for targeting the anticancer to treat brain cancer via nose-to-brain delivery.

Preparation and in- vitro Evaluation of Bioadhesive Vaginal Film of Tinidazole

Bioadhesive vaginal film is becoming a more effective and convenient dosage form compared to suppositories and gel for vaginal application as a method for the treatment of vaginal infections. This study aimed to prepare and characterize bioadhesive films of tinidazole to be used for vaginal delivery over a prolonged period to treat local infections. Fourteen formulas of tinidazole films were prepared by solvent evaporation method. Each film was composed of 10 mg tinidazole with different ratios and concentrations of a polymeric combination of polyvinyl alcohol/ polyvinyl pyrrolidone (PVA/PVP) or polyvinyl alcohol/ hydroxypropyl methylcellulose (PVA/HPMC) for formulas A1-A7 and B1-B7, respectively. The prepared films were evaluated for their physicochemical characteristics, content uniformity, swelling, mucoadhesive strength, mucoadhesive time, and drug release. All the prepared films were transparent, had a uniform thickness (0.1-0.15 mm), and exhibited sufficient flexibility with drug content uniformity. The mucoadhesive strength of films was in the range of 28 ± 0.2 to 75 ± 0.01 g. Films containing PVA/HPMC showed higher swelling and lower mucoadhesive strength than those containing PVA/PVP polymeric combination. The in vitro drug release study showed no significant differences (p > 0.05) among films containing PVA/PVP or PVA/HPMC polymeric combinations. Formulas A3 and B4 were considered as the optimal bioadhesive films containing 3% of PVA: PVP (4:1) and 4% of PVA: HPMC (2:1), respectively as they showed complete flexibility, acceptable mucoadhesive strength and time (43 ± 0.1, 45 ± 0.23 g and 30 ± 0.02, 34 ± 0.01 min, respectively) and prolonged drug release rate. In conclusion, films of formulas A3 and B4 possess the potential as a delivery system for tinidazole for the treatment of vaginal infections at the site of application.

DETERMINATION OF SOME PHARMACOKINETIC PROPERTIES OF ARTEMETHER-LUMEFANTRINE GRANULES IN ALBINO RATS

Aim and Objectives: Malaria is an infectious disease that is caused by plasmodium parasites which is rampant in Sahara Africa and children under 5 years of age are highly vulnerable to this infection by malaria. So the need for the formulation of dosage form for this population using naturally occurring excipients to replace imported ones being currently used by our local manufacturing industries in-order to formulate novel, readily available, affordable and effective antimalarial medicine for children. Methods: Using the local excipients and its hybrid, the formulated artemether-lumefantrine granules for oral suspension were administered to albino rats, blood samples were collected at predetermined time 0, 1.5, 3, 6, 9, 12, 15, 18, 21, and 24 h respectively and drug contents; artemether-lumefantrine were determined within the stipulated period. Results: Some pharmacokinetic parameters determined were; maximum concentration, Cmax, time to reach the maximum concentration, Tmax, half-life, t1/2, area under the curve, AUC, and mean residence time, MRT, which were for artemether-lumefantrine were 3.9, 3.4, μg/L; 3.2, 6.0 h; 12.5, 14 h; 75.8, 168.5 μg/L.h; 24, 24 h respectively, for the marketed artemether-lumefanthrine granules for oral suspension.4.1, 3.2 μg/L; 1.4, 3.0 h; 3.0, undefined h, 67.0, 65.7 μg/L. h; 18, 18 respectively for hybrid formulated artemether-lumefantrine granules for oral suspension and 3.1, 3.8 μg/L; 2.5, 12.5 h; 4.8, 15 h; 20.2, 281.6 μg/L .h; 18, 18 respectively for the extracted pectin formulated granules. Conclusion: Optimized formulated artemether-lumefantrine granules were superior to the marketed product in terms of pharmacokinetic values being closer to those of earlier workers. Peer Review History: Received 13 May 2024; Reviewed 16 July 2024; Accepted 22 August; Available online 15 September 2024 Academic Editor: Dr. Asia Selman Abdullah, Pharmacy institute, University of Basrah, Iraq, asia_abdullah65@yahoo.com Average Peer review marks at initial stage: 5.5/10 Average Peer review marks at publication stage: 7.0/10 Reviewers: Ahmad Najib, Universitas Muslim Indonesia, Makassar, Indonesia, ahmad.najib@umi.ac.id Dr. Sangeetha Arullappan, Universiti Tunku Abdul Rahman, Malaysia, sangeetha@utar.edu.my

Preparation of Aloysia citriodora (Lemon verbena) extract loaded lipid-nano capsules for topical antibacterial treatment

Nanocapsules have become a promising drug delivery approach for fighting bacterial infections. Extract from Aloysia citriodora (Lemon verbena), known for its biological activities and culinary applications, was investigated as a potential source for topical antibacterial treatment. The aim was to prepare and optimize lipid nanocapsules loaded with Aloysia citriodora extract, using both water and ethanol as solvents. The production, optimization, and characterization of these nanocapsules were conducted employing a Box-Behnken design to examine the impact of various factors on the polydispersity index, particle size, and entrapment efficiency. Assessments were made on solubility, stability, pH, and homogeneity, along with evaluations of in-vitro drug release, dermatokinetic properties, antioxidant activity, and antibacterial effects. The physical stability and quality of the nanocapsules were demonstrated with an average size of 104.6 nm and a polydispersity index (PDI) of 0.246. The encapsulation effectiveness was determined to be 87.08 %. In-vitro drug release studies revealed sustained release characteristics by the Korsmeyer Peppas model. Additionally, the formulation displayed significant antioxidant activity and promising antibacterial effects against Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus. Stability tests over ninety days showed that the formulation maintained structural integrity, consistent pH values and drug content, and good spreadability. The nanoformulation combined the benefits of Aloysia citriodora extract with the advantages of nanocapsule technology, offering a novel approach to addressing various pharmaceutical and antimicrobial challenges.

Novel pH-Responsive Structural Rearrangement of Myristic Acid-Conjugated Quetiapine Nanosuspension for Enhanced Long-Acting Delivery Performance.

Quetiapine myristate (QM), an ester-bonded lipophilic prodrug of quetiapine (QTP), is synthesized and converted into an amphiphilic structure in acidic pH to trigger a novel self-assembled QM nanosuspension (QMN). Following injection, this QMN rearranges within physiological pH to form nanoaggregates in structure, resulting in enhanced physicochemical properties and in vivo therapeutic performance without an initial burst release. The 200-nm-sized QMN exhibits less invasive injection, higher drug content, and better storage stability profile than conventional poly(lactide-co-glycolide) (PLGA) nanosuspensions containing QTP or QM. Following a single intramuscular injection to beagle dogs (35mg kg-1 QTP), QMN undergoes pH-responsive nanoaggregation to form the lipophilic prodrug, providing esterase-oriented sustained release for five weeks compared with the two-week period of PLGA nanosuspensions. Notably, QMN exhibits improved in vivo pharmacokinetic performance with long-acting delivery while minimizing issues associated with polymeric PLGA formulations, including the initial massive burst release, cellular toxicity, and adverse side effects. These results support the further development of QMN as a novel long-acting injectable to improve patient compliance and dosing frequency.