A new engineering process of biodegradable polymeric solid implants for ultra-long-acting drug delivery

Many active pharmaceutical ingredients (API) possess poor aqueous solubility and thus lead to poor bioavailability upon oral administration and topical application. Nanocrystals have a well-established, universal formulation approach to overcome poor solubility. Various nanocrystal-based products have entered the market for oral application. However, their use in dermal formulations is relatively novel. Previous studies confirmed that nanocrystals are a superior formulation principle to improve the dermal penetration of poorly soluble API. Other studies showed that nanocrystals can also be used to target the hair follicles where they create a drug depot, enabling long acting drug therapy with only one application. Very recent studies show that also the vehicle in which the nanocrystals are incorporated can have a tremendous influence on the pathway of the API and the nanocrystals. In order to elucidate the influence of the excipient in more detail, a systematic study was conducted to investigate the influence of excipients on the penetration efficacy of the formulated API and the pathway of nanocrystals upon dermal application. Results showed that already small quantities of excipients can strongly affect the passive dermal penetration of curcumin and the hair follicle targeting of curcumin nanocrystals. The addition of 2% ethanol promoted hair follicle targeting of nanocrystals and hampered passive diffusion into the stratum corneum of the API, whereas the addition of glycerol hampered hair follicle targeting and promoted passive diffusion. Propylene glycol was found to promote both pathways. In fact, the study proved that formulating nanocrystals to improve the bioefficacy of poorly soluble API upon dermal application is highly effective. However, this is only true, if the correct excipient is selected for the formulation of the vehicle. The study also showed that excipients can be used to allow for a targeted dermal drug delivery, which enables to control if API should be delivered via passive diffusion and/or as drug reservoir by depositing API in the hair follicles.

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A potential long-acting bictegravir loaded nano-drug delivery system for HIV-1 infection: A proof-of-concept study

Antiviral Research ◽

10.1016/j.antiviral.2019.04.007 ◽

2019 ◽

Vol 167 ◽

pp. 83-88 ◽

Cited By ~ 11

Author(s):

Subhra Mandal ◽

Pavan Kumar Prathipati ◽

Michael Belshan ◽

Christopher J. Destache

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Proof Of Concept ◽

Concept Study ◽

Nano Drug Delivery ◽

Long Acting ◽

Hiv 1

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From Immediate Release to Long Acting Drug Delivery Systems: What Do They Mean and Why Do They Matter?

Journal of Psychosocial Nursing and Mental Health Services ◽

10.3928/02793695-20170420-02 ◽

2017 ◽

Vol 55 (5) ◽

pp. 19-23 ◽

Cited By ~ 1

Author(s):

Laura G. Leahy

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Immediate Release ◽

Delivery Systems ◽

Long Acting

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Use of fibrin film as a carrier for drug delivery: A long-acting delivery system for pilocarpine into the eye.

Chemical and Pharmaceutical Bulletin ◽

10.1248/cpb.30.3405 ◽

1982 ◽

Vol 30 (9) ◽

pp. 3405-3407 ◽

Cited By ~ 18

Author(s):

SHOZO MIYAZAKI ◽

KUNIAKI ISHII ◽

MASAHIKO TAKADA

Keyword(s):

Drug Delivery ◽

Delivery System ◽

Long Acting

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Injectable Lipid-Based Depot Formulations: Where Do We Stand?

Pharmaceutics ◽

10.3390/pharmaceutics12060567 ◽

2020 ◽

Vol 12 (6) ◽

pp. 567 ◽

Cited By ~ 4

Author(s):

Lisa Rahnfeld ◽

Paola Luciani

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

In Vitro Release ◽

Delivery Systems ◽

The Body ◽

Solid Particles ◽

Depot Formulation ◽

Pharmaceutical Ingredients ◽

Long Acting

The remarkable number of new molecular entities approved per year as parenteral drugs, such as biologics and complex active pharmaceutical ingredients, calls for innovative and tunable drug delivery systems. Besides making these classes of drugs available in the body, injectable depot formulations offer the unique advantage in the parenteral world of reducing the number of required injections, thus increasing effectiveness as well as patient compliance. To date, a plethora of excipients has been proposed to formulate depot systems, and among those, lipids stand out due to their unique biocompatibility properties and safety profile. Looking at the several long-acting drug delivery systems based on lipids designed so far, a legitimate question may arise: How far away are we from an ideal depot formulation? Here, we review sustained release lipid-based platforms developed in the last 5 years, namely oil-based solutions, liposomal systems, in situ forming systems, solid particles, and implants, and we critically discuss the requirements for an ideal depot formulation with respect to the used excipients, biocompatibility, and the challenges presented by the manufacturing process. Finally, we delve into lights and shadows originating from the current setups of in vitro release assays developed with the aim of assessing the translational potential of depot injectables.

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Schizophrenia; A Review on Promising Drug Delivery Systems

Current Pharmaceutical Design ◽

10.2174/1381612826666200523173102 ◽

2020 ◽

Vol 26 (31) ◽

pp. 3871-3883

Author(s):

Ece Ö. Bülbül ◽

Ioannis D. Karantas ◽

Mehmet E. Okur ◽

Panoraia I. Siafaka ◽

Neslihan Ü. Okur

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Mental Illnesses ◽

Worldwide Population ◽

Second Generation Antipsychotics ◽

Schizophrenic Patients ◽

Long Acting ◽

First And Second Generation ◽

The Brain

Background: Schizophrenia belongs to mental illnesses affecting 1% of the worldwide population. Its therapy is still unmet; thus, researchers aimed to develop new pharmacological molecules which can improve its management. Methods: Moreover, the current typical and atypical antipsychotics should be formulated in more efficacious systems that can deliver the drug in the brain with as few side effects as possible. Further, the development of long-acting efficient drug delivery systems could be significant in minimizing frequent dosing which is nonpreferred to schizophrenics. Results: Herein, authors focused on current developments of antipsychotic medications used in schizophrenia management. Various studies, which include the use of first and second-generation antipsychotics, were analyzed according to their efficacy. In fact, in this review, oral, injectable, transdermal and intranasal formulations entrapped antipsychotics are presented to be valuable guidance for scientists to formulate more effective drug delivery systems for schizophrenic patients. Conclusions: This review aimed to assist researchers working on schizophrenia management by summarizing current medications and newly synthesized drug delivery systems recently found in the literature.

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