Alan Cowan: Buprenorphine from the bench to the bedside—Personal notes

In 2005, Bob Adams, the Chief Veterinarian at Johns Hopkins, wondered if sustained release technology could be used to improve postsurgical analgesia for animal medicine. Henry Brem, Director of the Hunterian Laboratories, had organized an international consortium to advance therapy for brain tumors and stroke. The Hunterian had over 20 years of experience with the safety and effectiveness of neutral lipids, phospholipids, carbohydrates, gels, polymers, and assorted devices for sustained-release drug delivery. We had the technology. What was the best pharmacology? Buprenorphine was the obvious analgesic. Reports of adverse events in the veterinary literature were rare.

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Formulation Optimization of Sustained Release Resinate Microcapsules of Tramadol Hydrochloride by Using 3/2 Factorial Design

International Journal of Pharmaceutical and Phytopharmacological Research ◽

10.24896/eijppr.2016621 ◽

2017 ◽

Vol 6 (2) ◽

pp. 57

Author(s):

Kamble Ravindra K. ◽

Chauhan Chetan S. ◽

Kamble Priyadarshani R. ◽

Naruka Pushpendra S.

Keyword(s):

Drug Delivery ◽

Ion Exchange ◽

Sustained Release ◽

Factorial Design ◽

Linear Regression Analysis ◽

Extended Period ◽

Multiple Linear Regression Analysis ◽

Water Soluble ◽

Tramadol Hydrochloride ◽

Release Drug

The main aim of the present work was to develop the microcapsules of tramadol hydrochloride for the oral sustained release drug delivery. Tramadol hydrochloride a BCS class I drug a centrally acting synthetic analgesic was complexed with Indion 254 ion exchange resin. The microcapsules were prepared by encapsulating the prepared resinates by o/o solvent evaporation technique. In the investigation 32 full factorial design was used to investigate the joint influence of two formulation variable amount of eudragit RS 100 and plasticized PEG 400. The results of multiple linear regression analysis indicated that for obtaining a sustained release drug delivery the optimum concentrations of both the plasticizer and coating solution to be used. The factorial models were used to prepare optimized microcapsules and optimized formulations showed sustained release profiles for the extended period of more than 12 hrs. From the present investigations concluded that resinate microcapsules of highly water soluble drug can provide controlled release of drug for extended period.Key Words: Tramadol hydrochloride, ion exchange resinate, microcapsules, sustained release

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Triptolide-nanoliposome-APRPG, a novel sustained-release drug delivery system targeting vascular endothelial cells, enhances the inhibitory effects of triptolide on laser-induced choroidal neovascularization

Biomedicine & Pharmacotherapy ◽

10.1016/j.biopha.2020.110737 ◽

2020 ◽

Vol 131 ◽

pp. 110737

Author(s):

Kunbei Lai ◽

Yingqin Li ◽

Yajun Gong ◽

Longhui Li ◽

Chuangxin Huang ◽

...

Keyword(s):

Drug Delivery ◽

Endothelial Cells ◽

Sustained Release ◽

Drug Delivery System ◽

Choroidal Neovascularization ◽

Delivery System ◽

Vascular Endothelial Cells ◽

Vascular Endothelial ◽

Inhibitory Effects ◽

Release Drug

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Incorporation of Levodopa into Biopolymer Coatings Based on Carboxylated Carbon Nanotubes for pH-Dependent Sustained Release Drug Delivery

Nanomaterials ◽

10.3390/nano8060389 ◽

2018 ◽

Vol 8 (6) ◽

pp. 389 ◽

Cited By ~ 6

Author(s):

Julia Tan ◽

Bullo Saifullah ◽

Aminu Kura ◽

Sharida Fakurazi ◽

Mohd Hussein

Keyword(s):

Carbon Nanotubes ◽

Drug Delivery ◽

Sustained Release ◽

Release Drug ◽

Ph Dependent ◽

Carboxylated Carbon Nanotubes

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Recent advances in intraocular sustained-release drug delivery devices

Drug Discovery Today ◽

10.1016/j.drudis.2019.05.031 ◽

2019 ◽

Vol 24 (8) ◽

pp. 1694-1700 ◽

Cited By ~ 13

Author(s):

Yiqi Cao ◽

Karen E. Samy ◽

Daniel A. Bernards ◽

Tejal A. Desai

Keyword(s):

Drug Delivery ◽

Sustained Release ◽

Release Drug ◽

Recent Advances ◽

Drug Delivery Devices

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Implementation of Quality by Design principles for the evolution of optimized sustained release drug delivery system

Drug Delivery Letters ◽

10.2174/2210303111666210421121812 ◽

2021 ◽

Vol 11 ◽

Author(s):

Lalit Singh ◽

Vijay Sharma

Keyword(s):

Mathematical Model ◽

Drug Delivery ◽

Sustained Release ◽

Drug Delivery System ◽

Delivery System ◽

Dosage Form ◽

Quality By Design ◽

Design Principles ◽

Release Drug

Aim: Aim of the present work is implementation of Quality by Design principles for the evolution of optimized sustained release drug delivery system Background: Quality by Design (QbD) approach refers to an advance approach to develop a optimized dosage form.QbD has become a vital modern scientific approach to develop a quality dosage form.In modern era of science researcher can develop a optimized dosage form with least effort, money and manpower. Objectives: Objective of research work wasthe successful development of optimized floating bioadhesive tablets of glipizide using floating-bioadhesive potential of cellulosic polymer and carbomersusing quality by design (QbD) approach. Method: Quality Target Product Profile (QTPP) of drug delivery system was defined as well as critical quality attributes (CQAs) were identified. A face centered central composite design (CCD) was utilized in assessing the impact of individual critical material attribute (CMA) like Hydro Propyl Methyl Cellulose K4M(HPMC K4M)and Carbopol 934P (CP 934P) and their interactions, using least experimentation. Formulations were developed and quantitative impact on CQAs was determined using mathematical model. The optimized formulation was obtained and characterized for in-vitro as well as in-vivo parameters. Results: A Fishikawa diagram and Failure Mode and Effect Analysis (FMEA) were performed to identify potential failure modes associated with the dosage form. The optimum formulation was embarked upon using mathematical model developed yielding desired CQAs followed for confirmation of data. Sustained release drug delivery system was successfully developed by using QbD approach. In-vivo X-ray imaging in rabbit and γ-scintigraphic study in manconfirmed the buoyant nature of the mucoadhesive floating tablet for 8 h in the upper gastrointestinal tract. Conclusion: Optimized formulation shows phenomenal floating, bioadhesive properties and drug release retardation characteristics, utilizing a mixture of cost-effective polymers Hence, QbD approach may be regarded as an important tool in development of floating bioadhesive CR dosage forms.

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Multivesicular Liposomes for the Sustained Release of Angiotensin I-Converting Enzyme (ACE) Inhibitory Peptides from Peanuts: Design, Characterization, and In Vitro Evaluation

Molecules ◽

10.3390/molecules24091746 ◽

2019 ◽

Vol 24 (9) ◽

pp. 1746 ◽

Cited By ~ 3

Author(s):

Ning Li ◽

Aimin Shi ◽

Qiang Wang ◽

Guoquan Zhang

Keyword(s):

Drug Delivery ◽

Zeta Potential ◽

Sustained Release ◽

Converting Enzyme ◽

Angiotensin I ◽

Ace Inhibitory Activity ◽

Angiotensin I Converting Enzyme ◽

Release Drug ◽

Ace Inhibitory

The multivesicular liposome (MVL) provides a potential delivery approach to avoid the destruction of the structure of drugs by digestive enzymes of the oral cavity and gastrointestinal system. It also serves as a sustained-release drug delivery system. In this study, we aimed to incorporate a water-soluble substance into MVLs to enhance sustained release, prevent the destruction of drugs, and to expound the function of different components and their mechanism. MVLs were prepared using the spherical packing model. The morphology, structure, size distribution, and zeta potential of MVLs were examined using an optical microscope (OM), confocal microscopy (CLSM), transmission electron cryomicroscope (cryo-EM) micrograph, a Master Sizer 2000, and a zeta sizer, respectively. The digestion experiment was conducted using a bionic mouse digestive system model in vitro. An in vitro release and releasing mechanism were investigated using a dialysis method. The average particle size, polydispersity index, zeta potential, and encapsulation efficiency are 47.6 nm, 1.880, −70.5 ± 2.88 mV, and 82.00 ± 0.25%, respectively. The studies on the controlled release in vitro shows that MVLs have excellent controlled release and outstanding thermal stability. The angiotensin I-converting enzyme (ACE) inhibitory activity of ACE-inhibitory peptide (AP)-MVLs decreased only 2.84% after oral administration, and ACE inhibitory activity decreased by 5.03% after passing through the stomach. Therefore, it could serve as a promising sustained-release drug delivery system.

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