Haigang Li, JiPeng Yao, Yong Guo, JingJing Huo, Haijuan Zhang, Zengtao Zhang, Jinlong Zhao & Chun Zhang
doi : 10.1208/s12249-023-02509-8
Volume 24, issue 1, January 2023
-Conotoxin CnIIIC (conotoxin, CTX)–loaded chitosan nanoparticles (CTX-NPs) were prepared using the ionic cross-linking method. The CTX-NPs were spherical and well with a polydispersity index of 0.292 ± 0.039, drug loading efficiency of 25.9 ± 1.2%, and encapsulation efficiency of 95.6 ± 1.3%.
Jirapornchai Suksaeree, Chaowalit Monton, Laksana Charoenchai, Natawat Chankana & Thaniya Wunnakup
doi : 10.1208/s12249-023-02514-x
Semha–Pinas (SHPN) is a Thai traditional herbal formula used as an expectorant. Its traditional dosage form is pills, which are dispersed in water before use.
Zhixing Lin, Kai Zheng, Mohammad A. Azad & Rajesh N. Davé
doi : 10.1208/s12249-023-02511-0
A highly porous additive, Neusilin®, with high adsorption capability is investigated to improve bulk properties, hence processability of spray-dried amorphous solid dispersions (ASDs). Griseofulvin (GF) is applied as a model BCS class 2 drug in ASDs.
Arti Mehandole, Nikita Walke, Srushti Mahajan, Mayur Aalhate, Indrani Maji, Ujala Gupta, Neelesh Kumar Mehra & Pankaj Kumar Singh
doi : 10.1208/s12249-023-02504-z
Amongst the several nano-drug delivery systems, lipid or polymer-based core–shell nanocapsules (NCs) have garnered much attention of researchers owing to its multidisciplinary properties and wide application.
Suyash M. Patil, Druva Sarika Barji, Tejashri Chavan, Kinjal Patel, Andrew J. Collazo, Vasudha Prithipaul, Aaron Muth & Nitesh K. Kunda
doi : 10.1208/s12249-023-02510-1
Tuberculosis (TB) is a contiguous airborne disease caused by Mycobacterium tuberculosis (M.tb), primarily affecting the human lungs. The progression of drug-susceptible TB to drug-resistant strains, MDR-TB and XDR-TB, has become a global challenge toward eradicating TB.
Manjusha Annaji, Nur Mita, Ishwor Poudel, Qi Wang, Brittany Tipton, R. Jayachandra Babu & Candace C. Lyman
doi : 10.1208/s12249-023-02513-y
Clomiphene citrate is the first-line treatment for women with abnormal or failed ovulation. Currently, it is available as oral tablets, and the parenteral formulation does not exist. In this study, we prepared clomiphene citrate-hydroxypropyl-β-cyclodextrin inclusion complex for its use in intravenous injection.
Dinesh Nyavanandi, Sagar Narala, Preethi Mandati, Abdullah Alzahrani, Praveen Kolimi, Ahmed Almotairy & Michael A. Repka
doi : 10.1208/s12249-023-02512-z
The current research is focused on investigating the suitability of the twin screw melt granulation (TSMG) approach for improving the solubility of a non-steroidal anti-inflammatory (NSAIDs) drug (ibuprofen), by developing granules using lipid surfactants.
Purva Pingle, Atul Mourya, Madhulika Namdeo, Katta Chanti Babu, Harithasree Veerabomma, Radheshyam Maurya, Pankaj Kumar Singh, Neelesh Kumar Mehra, Saurabh Srivastava & Jitender Madan
doi : 10.1208/s12249-023-02507-w
The utility of andrographolide (AN) in visceral leishmaniasis (VL) and cutaneous leishmaniasis (CL) is limited owing to poor solubility, hindered permeation, and unstable structure under physiological conditions.
Arnab Ganguly, Lisa Hardwick, Serguei Tchessalov, Steven L. Nail, Dan Dixon, Frank Kanka, Anthony Guidinas, T. N. Thompson, Cindy Reiter, Zakaria Yusoff, Ted Tharp, Joseph Azzarella, Prerona Sharma, Petr Kazarin, Alina Alexeenko & Michael J. Pikal
doi : 10.1208/s12249-023-02506-x
Best practices for performing freeze dryer equipment qualification are recommended, focusing on identifying methods to quantify shelf thermal uniformity (also known as “shelf surface uniformity�), equipment capability, and performance metrics of the freeze dryer essential to the pharmaceutical Quality by Design paradigm.
Shaaban K. Osman, Taher M. Yassin, Ahmed M. Mohammed, Abdallah M. Alfayomy, Ahmed A. Abdellatif, Wael A. Mahdi, Sultan Alshehri, Mohamed A. El Hamd, Hatem Sarhan & Mohammed A. Ibrahim
doi : 10.1208/s12249-022-02487-3
Tenoxicam (TX) is a non-steroidal anti-inflammatory agent that can be used to control pain in various ophthalmic lesions like cataracts, refractive surgery, and corneal abrasion. TX has a very slightly aqueous solubility of 0.072Â mg/mL resulting in difficulty to be formulated in ophthalmic solutions.
Humaira Sultana, Muhammad Naeem Aamir, Asadullah Madni, Masood ur Rehman, Afifa Shafiq, Jafir Hussain Shirazi, Sidra Hassan & Sumaira
doi : 10.1208/s12249-023-02499-7
Nanogel has attracted considerable attention as one of the most versatile drug delivery systems, especially for site-specific and/or time-controlled delivery of the chemotherapeutic agent.
Xiaoling Zheng, Jiahuan Zhu, Caihong Zheng, Zeng Tan, Zhonghua Ji, Jin Tao, Yunchun Zhao, Zhuwa Ji & Ying Hu
doi : 10.1208/s12249-022-02473-9
The objective of this study is to develop a new hepatitis B surface antigen (HBsAg) delivery system by coating soluble microneedle arrays with mannose-modified PLGA nanoparticles (MNPs).
Denise Tiemi Uchida & Marcos Luciano Bruschi
doi : 10.1208/s12249-023-02503-0
Wound healing is a dynamic process which involves stages of hemostasis, inflammation, proliferation and remodeling. Any error in this process results in abnormal wound healing, generating financial burdens for health systems and even affecting the physical and mental health of the patient.
Amna M. A. Makky, Eman S.El-leithy, Doaa Galaa Hussein & Abeer Khattab
doi : 10.1208/s12249-023-02500-3
Aminexil (AMX) is considered to be one of the most widely used hair growth promoters. Nanostructured lipid carriers (NLC) are employed to increase the permeation of both lipophilic and hydrophilic drugs.
Riya Mahar, Arpita Chakraborty, Nidhi Nainwal, Richa Bahuguna, Meenakshi Sajwan & Vikash Jakhmola
doi : 10.1208/s12249-023-02502-1
Pulmonary administration of biodegradable polymeric formulation is beneficial in the treatment of various respiratory diseases. For respiratory delivery, the polymer must be non-toxic, biodegradable, biocompatible, and stable.
Sunil Kumar Thota, Narendar Dudhipala, Venumadhav Katla & Kishan Veerabrahma
doi : 10.1208/s12249-022-02495-3
Efavirenz (EFV) is an anti-HIV drug with high dose and 40% oral bioavailability (BA). The aim was to improve the bioavailability by designing cationic solid SMEDDS. Solubility data, ternary phase diagrams, and central composite design were employed in design.
Hera Shams Khan, Fabienne Despres-Gnis, Cheryl L. M. Stults, James Mullis, Niran Nugara, Atish Sen & Lee Nagao
doi : 10.1208/s12249-022-02491-7
The presence of N-nitrosamines in drug products are currently an area of high regulatory and industry scrutiny, having been detected above acceptable regulatory levels in several solid oral drug products.
Liyao Liu, Jinju Nie & Letao Li
doi : 10.1208/s12249-022-02497-1
The current study aimed to improve the poor solubility of albendazole (ABZ) by means of phospholipid complexation, hence to improve its oral bioavailability. The solvent-evaporation method for ABZ-phospholipid complex (ABZ-PC) preparation was established for the first time. And a systematic optimization of preparation conditions of ABZ-PC was performed.
M. Scott Furness, Hong Cai, Sithamalli Chandramouli, Mariappan Chelliah, Xiao Hong Chen, Debasis Ghosh, Shaobo Liu, Sherita McLamore, Ramnarayan Randad & Meiyu Shen
doi : 10.1208/s12249-022-02498-0
FDA’s experience to date has shown that completion of stability data requirements is one of the most observed challenges for applicants of New Drug Applications (NDAs) with an expedited review designation.
Hussain Ali, Prakash Muthudoss, Manikandan Ramalingam, Lakshmi Kanakaraj, Amrit Paudel & Gobi Ramasamy
doi : 10.1208/s12249-022-02493-5
An increasingly large dataset of pharmaceutics disciplines is frequently challenging to comprehend. Since machine learning needs high-quality data sets, the open-source dataset can be a place to start.
J. W. Bezuidenhout, M. Aucamp, N. Stieger, W. Liebenberg & R. K. Haynes
doi : 10.1208/s12249-022-02490-8
For the purpose of establishing the optimum processing parameters and storage conditions associated with nanolipid formulations of the artemisinin derivative artesunate, it was necessary to evaluate the thermal stability and solubility profiles of artesunate in aqueous solutions at various temperatures and pH.
Shubham Gupta, Akhil Perla, Abhishek Roy, Jyotsna G. Vitore, Bharathi K, Sagar Salave, Dhwani Rana, Amit Sharma, Rajeshwari Rathod, Hemant Kumar & Derajram Benival
doi : 10.1208/s12249-022-02496-2
Migraine headaches are usually intolerable, and a quick-relief treatment remains an unmet medical need. Almotriptan malate is a serotonin (5-HT1B/1D) receptor agonist approved for the treatment of acute migraine in adults.
Wenjie Lu, Lingfei Yu, Lujun Wang, Songlin Liu, Manman Li, Zijun Wu, Shengqi Chen, Rongfeng Hu & Haiping Hao
doi : 10.1208/s12249-022-02402-w
Metformin hydrochloride enteric-coated capsule (MH-EC) is a commonly used clinical drug for the treatment of type 2 diabetes. In this study, we described a metformin hydrochloride mucosal nanoparticles enteric-coated capsule (MH-MNPs-EC) based on metformin hydrochloride chitosan mucosal nanoparticles (MH-CS MNPs) and its preparation method to improve the bioavailability and hypoglycemic effect duration of MH-EC.
Krishnayan Haldar, Mahesh S. Tirumkudulu, Ashwin Jain, Daniel O. Blackwood, Alfred Berchielli & Pankaj Doshi
doi : 10.1208/s12249-022-02474-8
Drying-induced cracks in tablet coatings are undesirable as they not only affect tablet’s appearance, but they may also interfere with its function.
Victor Hugo Pacagnelli Infante, Marcella Gabarra Almeida Leite & PatrÃcia M. B. G. Maia Campos
doi : 10.1208/s12249-022-02472-w
The film-forming effect is an important property of formulations for skin improvement and hair protection. Reflectance confocal microscopy, an advanced imaging technique, is an important tool for its evaluation.
Ryota Kimata, Naoki Yoshihara, Takayuki Terukina, Takanori Kanazawa & Hiromu Kondo
doi : 10.1208/s12249-022-02492-6
Drug-containing particles (DCPs) are frequently used as cores in the development of solid oral dosage forms. The wet layering technique, which is a typical approach for preparing DCPs, requires the use of solvents and a long manufacturing time.
Hiral Kapalatiya, Dhrumi Patel, Alok D. Singh & Sarika Wairkar
doi : 10.1208/s12249-022-02486-4
The current study aimed to improve the processability and oral bioavailability of itraconazole (ITZ) via spherical agglomeration. ITZ-spherical agglomerates (ITZ-SA) and ITZ-poloxamer 407-spherical agglomerates (ITZ-PLX-SA) were optimized using Box-Behnken design.
Pratik Kharat, Padakanti Sandeep Chary, Valamla Bhavana, Naveen Rajana, Geetanjali Devabattula, Chandraiah Godugu, Shashi Bala Singh & Neelesh Kumar Mehra
doi : 10.1208/s12249-022-02482-8
Essential oils consist of oxygenated structures of secondary metabolites of aromatic plants with anti-psoriatic activities. Tea tree oil (TTO) is an essential oil with good anti-microbial and anti-inflammatory properties, exhibiting reduced levels of IL-1, IL-8, and PGE 2.
Kajal Ghosal, Shreya Chatterjee, Sabu Thomas & Poulomi Roy
doi : 10.1208/s12249-022-02485-5
For progression of health care system, it has always been a challenge to the researchers for formulation to a type of advanced drug delivery system which will have less toxicity, targeted delivery and will be highly biodegradable.
Venugopala Swami Punati, Mahesh S. Tirumkudulu, Ashwin Jain, Daniel O. Blackwood, Alfred Berchielli & Pankaj Doshi
doi : 10.1208/s12249-022-02468-6
Immediate-release film coatings, also known as “non-functional� film coating, are applied to core tablets to improve product appearance and swallowability, impart taste-masking properties, improve handling and stability of the dosage form, and reduce exposure to active drug substance for caregivers.
Derya Arslan, Özlem Akbal Dağıstan, Olcay Sagirli, Lutfiye Mulazimoglu, Erdal Cevher & Ayca Yildiz-Pekoz
doi : 10.1208/s12249-022-02477-5
Buccal film formulations, including antifungal nystatin, anti-inflammatory agent hydrocortisone acetate, and local anesthetic lidocaine hydrochloride for pain relief, were developed.
Tipu Sultan, Shubhajit Paul, Enamul Hasan Rozin, Yin-Chao Tseng, Michael C. F. Bazzocchi & Cetin Cetinkaya
doi : 10.1208/s12249-022-02483-7
Due to their constituent powders, the materials of advanced compressed oral solid dosage (OSD) forms are micro-composites and strongly visco-elastic at macro- and micro-length scales.
Yangyan Chen, Yang Liu, Chuanbin Wu, Xin Pan & Tingting Peng
doi : 10.1208/s12249-022-02484-6
Azithromycin (AZI) is a commonly used antibiotic with extremely bitter taste that severely decreases the compliance of patients. Besides, the poor solubility of AZI in alkaline pH makes it difficult to be absorbed in the small intestine.
Preeti Dali & Pravin Shende
doi : 10.1208/s12249-022-02479-3
The objective of the current research study was to formulate the PEGylated lipid polymer hybrid nanoparticles of ergotamine and caffeine for intranasal administration with higher entrapment efficiency, better permeability, desirable controlled release pattern, and significant brain uptake in animal studies. A single-step nanoprecipitation method was employed in the processing of self-assembled hybrid nanoparticles constituting polymer PLGA, lipids soya lecithin, and DPPC with PEGylation using polyethylene glycol (PEG-2000).
Hamed Vaezi, Shahram Rabbani, Seyed Alireza Mortazavi, Mohammad Kamalinejad & Azadeh Haeri
doi : 10.1208/s12249-022-02476-6
This study aims to design and characterize berberine-loaded wafers for the treatment of chemotherapy-induced oral mucositis.
Srivalli N. Telikepalli, Michael J. Carrier, Dean C. Ripple, Greg Barnett, Ashwinkumar Bhirde, Donna Bolton, George M. Bou-Assaf, Erica Ferrari, Scott Leigh, Sophia Levitskaya-Seaman, Tim Menzen, Felix Nikels, Anna Riley, Miguel Saggu, Neha Sahni, Eric Vernooij & Klaus Wuchner
doi : 10.1208/s12249-022-02457-9
Visible protein-like particle standards may improve visual inspection and/or appearance testing practices used in the biotechnology industry.
Zahraa Hasan Falhi Al-Saedi, Zainab Thabit Salih, Kawther Khalid Ahmed, Rawnak Abdulrazzak Ahmed & Sawsan Abdulraheem Jasim
doi : 10.1208/s12249-022-02481-9
This study aims to formulate azithromycin oleogel to locally treat skin infections such as acne vulgaris and skin wound infection.
Shahjabeen Sharif, Saiqa Muneer, Tony Wang, Emad L. Izake & Nazrul Islam
doi : 10.1208/s12249-022-02480-w
This study investigated a systematic approach for producing ibuprofen (IBF) particles with leucine by wet milling. Using a high shear homogenizer, the particles size of the IBF was reduced.
Daila I. Hamdan, Nora Tawfeek, Riham A. El-Shiekh, Heba M. A. Khalil, Mohamed Y. Mahmoud, Alaa F. Bakr, Dalia Zaafar, Nawaal Farrag, Michael Wink & Assem Mohamed El-Shazly
doi : 10.1208/s12249-022-02478-4
Pollution is a worldwide environmental risk. Arsenic (As) is an environmental pollutant with a major health concern due to its toxic effects on multiple body organs, including the brain.
Guoliang Wang, Yanchao Li, Zhiguo Qin & Tao Liu
doi : 10.1208/s12249-022-02475-7
Nanotechnology and coamorphous are both advanced technologies that can effectively improve the solubility of drugs.
Preethi Mandati, Nagireddy Dumpa, Abdullah Alzahrani, Dinesh Nyavanandi, Sagar Narala, Honghe Wang, Suresh Bandari, Michael A. Repka, Sandip Tiwari & Nigel Langley
doi : 10.1208/s12249-022-02470-y
The main objective of the current research was to investigate the effect of tablet shapes (heart-shaped and round tablets) and infill densities (50% and 100%) on the drug release profiles of 3D printed tablets prepared by hot-melt extrusion paired with fused deposition modeling techniques.
Hao Wang, Qing Yao, Wenquan Zhu, Yang Yang, Chunsheng Gao, Cuiyan Han & Xiaoyang Chu
doi : 10.1208/s12249-022-02466-8
Chronic lead poisoning has become a major factor in global public health. Chelation therapy is usually used to manage lead poisoning.
Serguei Tchessalov, Evgenyi Shalaev, Bakul Bhatnagar, Steven Nail, Alina Alexeenko, Feroz Jameel, Jayasree Srinivasan, Michael Dekner, Ekneet Sahni, Stefan Schneid, Petr Kazarin, Orla McGarvey, Bert Van Meervenne, Vaibhav Kshirsagar, Paritosh Pande, Jens Philipp, Greg Sacha, Ke Wu, Joseph Azzarella, Gayathri Shivkumar & Shreyas Bhatt
doi : 10.1208/s12249-022-02463-x
The freeze-drying process scale-up and transfer remain a complicated and non-uniform practice. We summarized inefficient and good practices in these papers and provided some practical advice.
Benjamin M. Spence, Worth Longest, Rabijit Dutta, Mohammad A. M. Momin, Sarah Strickler & Michael Hindle
doi : 10.1208/s12249-022-02460-0
The objective of this study was to develop a new heated dryer system (HDS) for high efficiency lung delivery of nebulized aerosol and demonstrate performance with realistic in vitro testing for trans-nasal aerosol administration simultaneously with high-flow nasal cannula (HFNC) therapy and separately for direct oral inhalation (OI) of the aerosol.
Anusha V. Matadh, Deeksha Jakka, S. G. Pragathi, Srinath Rangappa, H. N. Shivakumar, Howard Maibach, N. M. Reena & S. Narasimha Murthy
doi : 10.1208/s12249-022-02471-x
Polymeric microneedles were prepared with Polyvinyl Pyrrolidone (PVP) K-30 using the mold casting technique. The core microneedles were coated with Eudragit E-100 by dip and spin method.
N. Başaran Mutlu-Ağardan, Serdar Tort, Şeyma Aydoğduoğlu & Merve Eylül Kıymacı
doi : 10.1208/s12249-022-02465-9
The aim of this study was formulating a new-generation antibacterial dressing in a form of polymer-based hybrid nanofiber-nanoparticles, effective on Gram-negative and Gram-positive bacteria using silver sulfadiazine (SSD), an FDA-approved topical antibiotic.
Dattatraya Yadav, Jignasa Savjani, Ketan Savjani, Aakash Kumar & Snehal Patel
doi : 10.1208/s12249-022-02467-7
The present research work attempted to improve the oral bioavailability of the antiviral drug Efavirenz (EFV) using a pharmaceutical cocrystallization technique. EFV comes under BCS-II and has extremely low water solubility, and results in low oral bioavailability.
Mohammed Elmowafy, Nabil K. Alruwaili, Naveed Ahmad, Abdulsalam M. Kassem & Mohamed F. Ibrahim
doi : 10.1208/s12249-022-02464-w
Mesoporous silica nanoparticles (MSNPs) have been proposed as a potential approach for stabilizing the amorphous state of poorly water-soluble actives.
Nirmayanti Nirmayanti, Alhidayah Alhidayah, Jessica Theodor Usman, Julika Fajrika Nur, Muh. Nur Amir & Andi Dian Permana
doi : 10.1208/s12249-022-02462-y
Due to the limitations of oral administration of valsartan, in this study, we aimed to develop thermosensitive hydrogel for sustained transdermal delivery and improved bioavailability of valsartan, which was further improved using solid microneedles.
Bhupendra Raj Giri & Mohammed Maniruzzaman
doi : 10.1208/s12249-022-02461-z
Three-dimensional (3D)-printed tablets prepared using powder-based printing techniques like selective laser sintering (SLS) typically disintegrate/dissolve and release the drug within a few minutes because of their inherent porous nature and loose structure.
Xiaoling Wang, Jiangyue Du, Feng Zhou, Qing Ye, Ying Chen, Dujuan Sun, Haimin Chen, Yuanyuan Lv & Xiaoyi Sun
doi : 10.1208/s12249-022-02469-5
Adequate delivery of therapeutic agents to their intended molecular targets is crucial in tumor therapy. Versatile drug carriers need to overcome the challenges coming from the systemic circulation, membrane barriers, and endo-lysosomal degradation.
Sayeed Mossadeq, Rajen Shah, Viraj Shah & Milind Bagul
doi : 10.1208/s12249-022-02455-x
The COVID-19 pandemic has proven to be an unprecedented health crisis in the human history with more than 5 million deaths worldwide caused to the SARS-CoV-2 and its variants
Lubna M. Abd El Wahab, Ebtessam A. Essa, Gamal M. El Maghraby & Mona F. Arafa
doi : 10.1208/s12249-022-02459-7
The aim of this study was to develop microemulsion (ME) formulation with possible phase transition into liquid crystals upon ocular application to enhance acetazolamide bioavailability.
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